[ CAS No. 1011459-26-9 ]

Name: 1011459-26-9|4,4,5,5-Tetramethyl-2-(2-methyl-4-(methylsulfonyl)phenyl)-1,3,2-dioxaborolane|97%
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Product Details of [ 1011459-26-9 ]

CAS No. :	1011459-26-9	MDL No. :	MFCD18732808
Formula :	C₁₄H₂₁BO₄S	Boiling Point :	-
Linear Structure Formula :	-	InChI Key :	NDJPXOFQIJCADG-UHFFFAOYSA-N
M.W :	296.19 g/mol	Pubchem ID :	59726032
Synonyms :

Safety of [ 1011459-26-9 ]

Signal Word:	Warning	Class:	N/A
Precautionary Statements:	P261-P305+P351+P338	UN#:	N/A
Hazard Statements:	H302-H315-H319-H335	Packing Group:	N/A
GHS Pictogram:

Application In Synthesis of [ 1011459-26-9 ]

* All experimental methods are cited from the reference, please refer to the original source for details. We do not guarantee the accuracy of the content in the reference.

Downstream synthetic route of [ 1011459-26-9 ]

[ 1011459-26-9 ] Synthesis Path-Downstream 1~16

1
[ 99769-28-5 ]
[ 73183-34-3 ]
[ 1011459-26-9 ]

Yield	Reaction Conditions	Operation in experiment
68%	With (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride; potassium acetate In ethyl acetate; N,N-dimethyl-formamide at 80℃; for 22h; Inert atmosphere;	39 To a solution of 1-bromo-4-methanesulfonyl-2-methylbenzene (2.38 g, 9.55 mmol) in N,N-dimethylformamide (48 mL) under nitrogen was added pinacol diborane (3.64 g, 14.33 mmol), potassium acetate (4.68 g, 47.75 mmol) and Pd(dppf)2Cl2 (0.69 g, 0.95 mmol). The reaction was heated at 80° C. for 22 h. After that time the reaction was cooled to rt, concentrated under reduced pressure and re-dissolved in ethyl acetate. A solution of 2M HCl was added and the precipitated solids were removed by filtration. The filtrate was extracted with ethyl acetate (2×100 mL). The combined organic phase was washed with brine, dried over Na2SO4 and concentrated under reduced pressure. The product was purified by flash column chromatography (silica gel, 90:10 Hexanes/ethyl acetate) to give 4,4,5,5-tetramethyl-2-(2-methyl-4-(methylsulfonyl)phenyl)-1,3,2-dioxaborolane (1.92 g, 68%) as a white solid: 1H NMR (400 MHz, CDCl3) δ 7.94 (d, J=8.21 Hz, 1H), 7.69-7.74 (m, 2H), 3.03 (s, 3H), 2.62 (s, 3H), 1.36 (s, 12H).
	With potassium acetate In N,N-dimethyl-formamide at 80℃; for 16h;	11.6 Step 6: A solution of l-bromo-2-methyl-4-(methylsulfonyl)benzene (0.693 g, 2.78 mmol), bis(pinacolato)diboron (1.06 g, 4.17 mmol), dichloro[l,l'- bis(diphenylphosphino)ferrocene]palladium (II) dichloromethane adduct (0.204 g, 0.278 mmol) and potassium acetate (1.37 g, 13.9 mmol) in 14 mL of DMF was stirred and heated at 80°C for 16 hours. Then the reaction mixture was cooled to RT and concentrated. The crude material was taken up in EtOAc and 2M HCl and filtered. The layers were separated and the aqueous layer was extracted with EtOAc and the combined organic layers were washed with NaCl (sat.), dried over sodium sulfate, filtered and concentrated to give 1.55 g of a brown oil. The crude material was purified by silica gel chromatography (3/1 Hex/EtOAc) to afford 480 mg of 454.5,5-tetramethyl-2-(2-methyl-4- (methylsulfonyl)phenyl)-l,3,2-dioxaborolane as a white solid. MS+=297.1 (M+H)
	With dichloro(1,1'-bis(diphenylphosphanyl)ferrocene)palladium(II)*CH₂Cl₂; potassium acetate In 1,4-dioxane for 2.5h; Inert atmosphere;	70 EXAMPLE 70 (7R, 1 4R)- 1 -(difluoromethoxy)- 11 -[2-methyl-4-(methylsulfonyl)phenyll-6,7-dihydro-7,1 4-methanobenzimidazo [1 ,2-bl [2,5 lbenzodiazocin-5 (1 411)-one (1-bromo-4-methanesulfonyl-2-methylbenzene (483 mg, 1.86 mmol), bis(pinacolato)diboron (525 mg, 2.0 mmol), and potassium acetate (369 mg, 3.7 mmol) were dissolved in 1,4-dioxane (15 mL) and the mixture degassed thoroughly with nitrogen. 1,1 ‘-bis(diphenylphosphino)ferrocene-palladium(II)dichloride dichloromethanecomplex (38 mg, 0.05 mmol) was then added and the mixture heated for 2.5 hours under nitrogen. The reaction mixture was separated between EtOAc (25 mL) and water (25 mL). The organic layer was passed through a phase separator and evaporated in vacuo.The crude product was engaged in a Suzuki reaction with Example 11 (350 mg, 0.93 mmol), tricyclohexylphosphonium tetrafluoroborate (42 mg, 0.11 mmol), tris(dibenzylideneacetone)-dipalladium(0) (56 mg, 0.060 mmol), and K3P04 (592 mg, 2.79 mmol) in dioxane (5m1) plus 2 drops of water. The mixture was heated in microwave for 18 hours at 110 degrees. After this time the reaction mixture was separated between EtOAc (25 mL) and water (25 mL) and the organic layer was passed through a phaseseparator and evaporated in vacuo. The resultant residue was then purified by flash chromatography (Si02, 0 to 100% EtOAc in DCM and then 1 to 10% MeOH in EtOAc) to obtain mostly pure product (350 mg as brown solid 90% pure). Further purification by flash chromatography on silica gel 1-10% MeOH in DCM gave the title compound as off white powder (45 mg, 10%).1H NMR (300 MHz, DMSO-d6) ö 9.15 (d, J= 6.9 Hz, 1H), 8.31 - 8.18 (m, 1H), 7.89 (d,J= 2.0 Hz, 1H), 7.87 - 7.65 (m, 2H), 7.59 - 7.38 (m, 4H), 7.45 (t, J= 73 Hz, 1H), 7.36 -7.15 (m, 1H), 6.31 (d, J 7.1 Hz, 1H), 4.89 (t, J= 6.7 Hz, 1H), 3.49 (dt, J= 13.6, 7.1 Hz,1H), 3.26 (s, 3H), 2.74 (d, J= 13.4 Hz, 1H), 2.30 (s, 3H). LCMS basic Method 5 (ES+)RT 1.83 mm, 510 (M+H).

	With (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride; potassium acetate In 1,4-dioxane at 105℃; for 1h; Inert atmosphere;	A mixture of l-bromo-2-methyl-4-methylsulfonyl-benzene (170 mg, 648 pmol, 1.00 equiv), potassium acetate (127 mg, 1.30 mmol, 2.00 equiv), Pd(dppf)Cl2 (47.4 mg, 64.8 pmol, 0.100 equiv) and 4, 4, 5, 5-tetramethyl-2-(4, 4, 5, 5-tetramethyl-l, 3, 2-dioxaborolan-2-yl) -1, 3, 2- dioxaborolane (247 mg, 972 pmol, 1.50 equiv) in dioxane (3.00 mL) was purged with nitrogen. The resultant reaction mixture was stirred at 105 °C for 1 h. The mixture was filtered and concentrated under reduced pressure to give a residue. The crude material was purified by prep-TLC (petroleum ether / ethyl acetate, 5 / 1) to afford 4, 4, 5, 5-tetramethyl-2-(2-methyl-4- methylsulfonyl-phenyl)-l, 3, 2-dioxaborolane (110 mg, 338 pmol, 52.1% yield, 90.9% purity) as a colorless oil. LCMS [M+l]: 296.9.
	With (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride; potassium acetate In 1,4-dioxane at 105℃; for 1h; Inert atmosphere;	A mixture of 1-bromo-2-methyl-4-methylsulfonyl-benzene (170 mg, 648 μmol, 1.00 equiv), potassium acetate (127 mg, 1.30 mmol, 2.00 equiv), Pd(dppf)Cl2 (47.4 mg, 64.8 μmol, 0.100 equiv) and 4,4,5,5-tetramethyl-2-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl) -1,3,2- dioxaborolane (247 mg, 972 μmol, 1.50 equiv) in dioxane (3.00 mL) was purged with nitrogen. The resultant reaction mixture was stirred at 105 °C for 1 h. The mixture was filtered and concentrated under reduced pressure to give a residue. The crude material was purified by prep-TLC (petroleum ether / ethyl acetate, 5 / 1) to afford 4,4,5,5-tetramethyl-2- (2-methyl-4-methylsulfonyl-phenyl)-1,3,2-dioxaborolane (110 mg, 338 μmol, 52.1% yield, 90.9% purity) as a colorless oil. LC-MS [M+1]: 296.9.
	With (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride; potassium acetate In 1,4-dioxane at 105℃; for 1h; Inert atmosphere;	[0297] A mixture of 1-bromo-2-methyl-4-methylsulfonylbenzene (170 mg, 648 mol, 1.00 equiv), potassium acetate (127 mg, 1.30 mmol, 2.00 equiv), Pd(dppf)Cl2 (47.4 mg, 64.8 mol, 0.100 equiv) and 4,4,5,5-tetramethyl-2-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl) - 1,3,2- dioxaborolane (247 mg, 972 mol, 1.50 equiv) in dioxane (3.00 mL) was purged with nitrogen. The resultant reaction mixture was stirred at 105 °C for 1 h. The mixture was filtered and concentrated under reduced pressure to give a residue. The crude material was purified by prep-TLC (petroleum ether / ethyl acetate, 5 / 1) to afford 4,4,5,5-tetramethyl-2-(2-methyl-4-methylsulfonylphenyl)-1,3,2-dioxaborolane (110 mg, 338 mol, 52.1 % yield, 90.9% purity) as a colorless oil. LCMS [M+1]: 296.9.

Reference： [1]Current Patent Assignee: ZENITH CAPITAL CORP - US2014/140956, 2014, A1 Location in patent: Paragraph 0786
[2]Current Patent Assignee: AMGEN INC - WO2008/30466, 2008, A1 Location in patent: Page/Page column 56
[3]Current Patent Assignee: SANOFI; UCB - WO2016/50975, 2016, A1 Location in patent: Page/Page column 275; 276
[4]Current Patent Assignee: MIRATI THERAPEUTICS, INC. - WO2019/152419, 2019, A1 Location in patent: Paragraph 0302; 0306
[5]Current Patent Assignee: MIRATI THERAPEUTICS, INC. - WO2020/219448, 2020, A1 Location in patent: Paragraph 0356
[6]Current Patent Assignee: MIRATI THERAPEUTICS, INC. - WO2020/247475, 2020, A1 Location in patent: Paragraph 0297

2
[ 1011459-26-9 ]
[ 1221270-31-0 ]
[ 1221269-96-0 ]

Yield	Reaction Conditions	Operation in experiment
	With sodium carbonate In 1,2-dimethoxyethane; ethanol; water at 140℃; for 0.166667h; Microwave irradiation;	2.3 Step 3 : N-(4-FluorophenvD- 1 -(2-methyl-4-(methylsulfonyl)phenyl)phthalazin-6-amine; A mixture of l-chloro-N-(4-fluorophenyl)phthalazin-6-amine (200 mg, 0.73 mmol), 4,4,5,5-tetramethyl-2-(2-methyl-4-(methylsulfonyl)phenyl)-l,3,2-dioxaborolane (260 mg, 0.88 mmol), trans-dichlorobis(triphenylphosphine)palladium (II) (26 mg, 0.037 mmol), and sodium carbonate (232 mg, 2.19 mmol) in a 7:2:3 mixture of DME, EtOH and water (3 mL) was heated at 140 0C for 10 min in the Emrys Optimizer microwave. After cooling to RT, the mixture was diluted with saturated aqueous solution OfNaHCO3 and extracted with CH2Cl2 (3X). The combined organics were dried over Na2SOzJ, filtered and concentrated. The residue was purified using column chromatography (0-75% acetone in hexanes) to yield the title compound as a tan crystalline solid. MS (ESI, pos. ion) m/z: 408.1 (M+l).

Reference： [1]Current Patent Assignee: AMGEN INC - WO2010/42649, 2010, A2 Location in patent: Page/Page column 39-40

3
[ 1011459-26-9 ]
[ 1610372-27-4 ]
[ 1610373-36-8 ]

Yield	Reaction Conditions	Operation in experiment
77%	With tetrakis(triphenylphosphine) palladium⁽⁰⁾; sodium carbonate In ethanol; toluene at 100℃; for 22h; Inert atmosphere;	39 A mixture of 6-bromo-5-(2-((tert-butyldimethylsilyl)oxy)ethoxy)picolinaldehyde (1.21 g, 3.37 mmol), 2-(4-methanesulfonyl-2-methyl-phenyl)-4,4,5,5-tetramethyl-[1,3,2]dioxaborolane (1.0 g, 3.37 mmol) and 2M Na2CO3 solution (6.74 mL, 13.48 mmol) in toluene (12 mL) and ethanol (6 mL) was degassed with nitrogen. Pd(PPh3)4 (0.39 g, 0.337 mmol) was added and the reaction heated at 100° C. for 22 h. After that time the reaction was cooled to rt, diluted with brine and extracted with ethyl acetate (2×100 mL). The combined organic phase was dried over Na2SO4 and concentrated under reduced pressure. The product was purified by flash column chromatography (silica gel, 90:10 hexanes/ethyl acetate to 70:30 hexanes/ ethyl acetate) to give 5-(2-((tert-butyldimethylsilyl)oxy)ethoxy)-6-(2-methyl-4-(methylsulfonyl)phenyl)picolinaldehyde (1.42 g, 77%) as an orange oil: 1H NMR (400 MHz, CDCl3) δ 10.10 (s, 1H), 8.14 (d, J=8.60 Hz, 1H), 7.91-8.00 (m, 2H), 7.63 (d, J=7.82 Hz, 1H), 7.59 (d, J=8.60 Hz, 1H), 4.23-4.28 (m, 2H), 3.92-3.98 (m, 2H), 3.16 (s, 3H), 2.38 (s, 3H), 0.89 (s, 9H), 0.00 (s, 6H).

Reference： [1]Current Patent Assignee: ZENITH CAPITAL CORP - US2014/140956, 2014, A1 Location in patent: Paragraph 0787

4
[ 90532-02-8 ]
[ 1011459-26-9 ]

Yield	Reaction Conditions	Operation in experiment
	Multi-step reaction with 2 steps 1: Oxone / water; methanol / 18 h / 0 - 20 °C 2: potassium acetate; (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride / N,N-dimethyl-formamide; ethyl acetate / 22 h / 80 °C / Inert atmosphere
	Multi-step reaction with 2 steps 1: 3-chloro-benzenecarboperoxoic acid / dichloromethane / 2 h / 0 - 25 °C 2: potassium acetate; (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride / 1,4-dioxane / 1 h / 105 °C / Inert atmosphere
	Multi-step reaction with 2 steps 1: 3-chloro-benzenecarboperoxoic acid / dichloromethane / 2 h / 0 - 25 °C 2: potassium acetate; (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride / 1,4-dioxane / 1 h / 105 °C / Inert atmosphere

Reference： [1]Current Patent Assignee: ZENITH CAPITAL CORP - US2014/140956, 2014, A1
[2]Current Patent Assignee: MIRATI THERAPEUTICS, INC. - WO2019/152419, 2019, A1
[3]Current Patent Assignee: MIRATI THERAPEUTICS, INC. - WO2020/219448, 2020, A1 Current Patent Assignee: MIRATI THERAPEUTICS, INC. - WO2020/247475, 2020, A1

5
[ 1011459-26-9 ]
[ 1610372-65-0 ]

Yield	Reaction Conditions	Operation in experiment
	Multi-step reaction with 2 steps 1: tetrakis(triphenylphosphine) palladium⁽⁰⁾; sodium carbonate / ethanol; toluene / 22 h / 100 °C / Inert atmosphere 2: toluene-4-sulfonic acid; sodium hydrogensulfite / N,N-dimethyl acetamide / 18 h / 120 °C

Reference： [1]Current Patent Assignee: ZENITH CAPITAL CORP - US2014/140956, 2014, A1

6
[ 1011459-26-9 ]
[ 1610373-51-7 ]

Yield	Reaction Conditions	Operation in experiment
	Multi-step reaction with 3 steps 1: tetrakis(triphenylphosphine) palladium⁽⁰⁾; sodium carbonate / ethanol; toluene / 22 h / 100 °C / Inert atmosphere 2: toluene-4-sulfonic acid; sodium hydrogensulfite / N,N-dimethyl acetamide / 18 h / 120 °C 3: phosphorus tribromide / N,N-dimethyl-formamide / 2 h / 60 °C

Reference： [1]Current Patent Assignee: ZENITH CAPITAL CORP - US2014/140956, 2014, A1

7
[ 1011459-26-9 ]
[ 1610372-71-8 ]

Yield	Reaction Conditions	Operation in experiment
	Multi-step reaction with 4 steps 1: tetrakis(triphenylphosphine) palladium⁽⁰⁾; sodium carbonate / ethanol; toluene / 22 h / 100 °C / Inert atmosphere 2: toluene-4-sulfonic acid; sodium hydrogensulfite / N,N-dimethyl acetamide / 18 h / 120 °C 3: phosphorus tribromide / N,N-dimethyl-formamide / 2 h / 60 °C 4: dimethyl sulfoxide / 18 h / 50 °C / Sealed tube

Reference： [1]Current Patent Assignee: ZENITH CAPITAL CORP - US2014/140956, 2014, A1

8
[ 1011459-26-9 ]
(7R,14R)-11-chloro-1-(difluoromethoxy)-6,7-dihydro-7,14-methanobenzimidazo[1,2-b][2,5]benzodiazocin-5(14H)-one [ No CAS ]
(7R,14R)-1-(difluoromethoxy)-11-[2-methyl-4-(methylsulfonyl)phenyl]-6,7-dihydro-7,14-methanobenzimidazo[1,2-b][2,5]benzodiazocin-5(14H)-one [ No CAS ]

Yield	Reaction Conditions	Operation in experiment
10%	With potassium phosphate; tris-(dibenzylideneacetone)dipalladium⁽⁰⁾; tricyclohexylphosphine tetrafluoroborate In 1,4-dioxane; water at 110℃; for 18h; Microwave irradiation;	70 EXAMPLE 70 (7R, 1 4R)- 1 -(difluoromethoxy)- 11 -[2-methyl-4-(methylsulfonyl)phenyll-6,7-dihydro-7,1 4-methanobenzimidazo [1 ,2-bl [2,5 lbenzodiazocin-5 (1 411)-one (1-bromo-4-methanesulfonyl-2-methylbenzene (483 mg, 1.86 mmol), bis(pinacolato)diboron (525 mg, 2.0 mmol), and potassium acetate (369 mg, 3.7 mmol) were dissolved in 1,4-dioxane (15 mL) and the mixture degassed thoroughly with nitrogen. 1,1 ‘-bis(diphenylphosphino)ferrocene-palladium(II)dichloride dichloromethanecomplex (38 mg, 0.05 mmol) was then added and the mixture heated for 2.5 hours under nitrogen. The reaction mixture was separated between EtOAc (25 mL) and water (25 mL). The organic layer was passed through a phase separator and evaporated in vacuo.The crude product was engaged in a Suzuki reaction with Example 11 (350 mg, 0.93 mmol), tricyclohexylphosphonium tetrafluoroborate (42 mg, 0.11 mmol), tris(dibenzylideneacetone)-dipalladium(0) (56 mg, 0.060 mmol), and K3P04 (592 mg, 2.79 mmol) in dioxane (5m1) plus 2 drops of water. The mixture was heated in microwave for 18 hours at 110 degrees. After this time the reaction mixture was separated between EtOAc (25 mL) and water (25 mL) and the organic layer was passed through a phaseseparator and evaporated in vacuo. The resultant residue was then purified by flash chromatography (Si02, 0 to 100% EtOAc in DCM and then 1 to 10% MeOH in EtOAc) to obtain mostly pure product (350 mg as brown solid 90% pure). Further purification by flash chromatography on silica gel 1-10% MeOH in DCM gave the title compound as off white powder (45 mg, 10%).1H NMR (300 MHz, DMSO-d6) ö 9.15 (d, J= 6.9 Hz, 1H), 8.31 - 8.18 (m, 1H), 7.89 (d,J= 2.0 Hz, 1H), 7.87 - 7.65 (m, 2H), 7.59 - 7.38 (m, 4H), 7.45 (t, J= 73 Hz, 1H), 7.36 -7.15 (m, 1H), 6.31 (d, J 7.1 Hz, 1H), 4.89 (t, J= 6.7 Hz, 1H), 3.49 (dt, J= 13.6, 7.1 Hz,1H), 3.26 (s, 3H), 2.74 (d, J= 13.4 Hz, 1H), 2.30 (s, 3H). LCMS basic Method 5 (ES+)RT 1.83 mm, 510 (M+H).

Reference： [1]Current Patent Assignee: SANOFI; UCB - WO2016/50975, 2016, A1 Location in patent: Page/Page column 275; 276

Yield	Reaction Conditions	Operation in experiment
	With (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride; potassium acetate In 1,4-dioxane at 90℃; for 4h; Inert atmosphere;	B29 Intermediate B1 General procedure: Intermediate B1 (0351) A mixture of B1.4 (12 g, 64 mmol), bis(pinacolato)diboron (22.8 g, 89.6 mmol, 1.4 eq), KOAc (18.8 g, 192 mmol, 3.0 eq), and Pd(dppf)Cl2 (2.34 g, 3.2 mmol) in 200 mL of anhydrous dioxane was heated at 90° C. and stirred for 4 h under N2. The solvent was removed under reduced pressure, the residue was diluted with 300 mL mixed slovent (PE:EA=4:1), filtered and concentrated. The crude product was purified by flash column chromatography (PE:EA=2:1 to 1:1) to give the title compound (10 g, 66%) as a yellow oil. LC-MS: [M+H]+=235.1.
	With (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride; potassium acetate In 1,4-dioxane at 90℃; for 4h; Inert atmosphere;	Intermediate BI General procedure: A mixture of B1.4 (12 g, 64 mmol), bis(pinacolato)diboron (22.8 g, 89.6 mmol, 1.4 eq), KOAc (18.8 g, 192 mmol, 3.0 eq), and Pd(dppt)C12 (2.34 g, 3.2 mmol) in 200 mL of anhydrous dioxane was heated at 90 °C and stirred for 4 h under N2. The solvent was removed under reduced pressure, the residue was diluted with 300mL mixed slovent (PE:EA = 4:1), filtered and concentrated. The crude product was purified by flash column chromatography (PE:EA = 2:1 to 1:1) to give the title compound (10 g, 66%) as a yellow oil. LC-MS: [M+H] = 235.1.

10
[ 452-63-1 ]
[ 1011459-26-9 ]

Yield	Reaction Conditions	Operation in experiment
	Multi-step reaction with 3 steps 1: N,N-dimethyl-formamide / 12 h / 50 °C 2: 3-chloro-benzenecarboperoxoic acid / dichloromethane / 2 h / 0 - 25 °C 3: potassium acetate; (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride / 1,4-dioxane / 1 h / 105 °C / Inert atmosphere
	Multi-step reaction with 3 steps 1: N,N-dimethyl-formamide / 12 h / 50 °C 2: 3-chloro-benzenecarboperoxoic acid / dichloromethane / 2 h / 0 - 25 °C 3: potassium acetate; (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride / 1,4-dioxane / 1 h / 105 °C / Inert atmosphere
	Multi-step reaction with 3 steps 1: N,N-dimethyl-formamide / 12 h / 50 °C 2: 3-chloro-benzenecarboperoxoic acid / dichloromethane / 2 h / 0 - 25 °C 3: potassium acetate; (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride / 1,4-dioxane / 1 h / 105 °C / Inert atmosphere

Reference： [1]Current Patent Assignee: MIRATI THERAPEUTICS, INC. - WO2019/152419, 2019, A1
[2]Current Patent Assignee: MIRATI THERAPEUTICS, INC. - WO2020/219448, 2020, A1
[3]Current Patent Assignee: MIRATI THERAPEUTICS, INC. - WO2020/247475, 2020, A1

11
[ 1011459-26-9 ]
8-bromo-5-(((5-fluoro-2,3-dihydrobenzofuran-4-yl)methyl)amino)imidazo[1,2-c]pyrimidine-2-carbonitrile [ No CAS ]
5-(((5-fluoro-2,3-dihydrobenzofuran-4-yl)methyl)amino)-8-(2-methyl-4-(methylsulfonyl)phenyl)imidazo[1,2-c]pyrimidine-2-carbonitrile [ No CAS ]

Yield	Reaction Conditions	Operation in experiment
51 mg	With (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride; sodium hydrogencarbonate In 1,4-dioxane; water at 100℃; for 2h; Inert atmosphere;	87 5-(((5-fluoro-2, 3 -dihydrobenzofuran-4-yl)m ethyl )amino)-8-(2 -methyl -4- (methylsulfonyl)phenyl)imidazo[l , 2-c]pyrimidine-2-carbonitrile A mixture of 8-bromo-5-(((5-fluoro-2, 3-dihydrobenzofuran-4- yl)methyl)amino)imidazo[l , 2-c]pyrimidine-2-carbonitrile (90.0 mg, 231 pmol, 1.00 equiv), 1, 3-dimethyl-5-(4, 4, 5, 5-tetramethyl-l, 3, 2-dioxaborolan-2-yl)pyrazole (103 mg, 463 pmol, 2.00 equiv), Pd(dppf)Cl2 (16.9 mg, 23.1 pmol, 0.100 equiv), sodium bicarbonate (58.4 mg, 695 pmol, 27.0 pL, 3 equiv) in dioxane (6.00 mL) and water (3.00 mL) was purged with nitrogen. The resultant mixture was stirred at 100 °C for 2 h under an atmosphere of nitrogen. Water (8.00 mL) was added and the mixture was extracted with ethyl acetate (8.00 mL c 3). The combined organic layer was concentrated in vacuo to give a residue. The crude material was purified by Prep-HPLC (column: Phenomenex Synergi C 18 15025 10 pm;mobile phase: [water(0. l%TFA)-ACN];B%: 33%-63%, l3min) to 8-(l, 3-dimethyl-lH-pyrazol-5-yl)-5-(((5- fluoro-2, 3-dihydrobenzofuran-4-yl)methyl)amino)imidazo[l, 2-c]pyrimidine-2-carbonitrile (51.0 mg, 120 pmol, 52.0% yield, 95.4% purity) as a white solid. LC-MS: [M+l] 404. 1H NMR (400 MHz, DMSO-i) d = 8.92 (s, 1H), 8.64 (br t , j= 4.8 Hz, 1H), 7.86 (s, 1H), 6.99 - 6.91 (m, 1H), 6.71 (dd, j= 4.0, 8.8 Hz, 1H), 6.23 (s, 1H), 4.72 (br d, j= 4.4 Hz, 2H), 4.55 (t, J= 8.8 Hz, 2H), 3.67 (s, 3H), 3.31 (t, J= 8.8 Hz, 2H), 2.18 (s, 3H).
	With dichloro(1,1'-bis(diphenylphosphanyl)ferrocene)palladium(II)*CH₂Cl₂; sodium hydrogencarbonate In 1,4-dioxane; water at 95℃; for 1h; Inert atmosphere;	13.A 2-(aminomethyl)-N-((5-fluoro-2,3-dihydrobenzofuran-4-yl)methyl)-8-(2-methyl-4-(methylsulfonyl)phenyl)imidazo[1,2-c]pyrimidin-5-amine [0436] Step A: To a solution of 8-bromo-5-(((5-fluoro-2,3-dihydrobenzofuran-4-yl)methyl)amino)imidazo[1,2-c]pyrimidine-2-carbonitrile (121 mg, 302. mol, 1.00 eq) and 4,4,5,5-tetramethyl-2-(2-methyl-4-(methylsulfonyl)phenyl)-1,3,2-dioxaborolane (150 mg, 456 mol, 1.50 eq), sodium bicarbonate (76.0 mg, 905 mol, 35.2 L, 3.00 eq) in a mixture solvent of dioxane (1.70 mL) and water (0.30 mL) was added Pd(dppf)Cl2.CH2Cl2 (25.0 mg, 30.6 mol, 0.10 eq). The mixture was stirred at 95 °C for 1 hour under a nitrogen atmosphere. The reaction mixture was evaporated to give a residue, the residue was purified by prep-TLC (SiO2, dichloromethane: methanol = 20:1) to give 5-(((5-fluoro-2,3-dihydrobenzofuran-4-yl)methyl)amino)-8-(2-methyl-4-(methylsulfonyl)phenyl)imidazo[1,2-c]pyrimidine-2-carbonitrile (80.0 mg, 49.4 % yield, 89.0% purity) as a light yellow solid. LCMS [M+1]: 478.1. [0437] 1H NMR (400MHz, DMSO-d6) d = 8.93 (s, 1H), 8.58 (t, J = 5.2 Hz, 1H), 7.89 (d, J = 1.2 Hz, 1H), 7.83 - 7.78 (m, 2H), 7.58 (d, J = 8.4 Hz, 1H), 7.04 - 6.89 (m, 1H), 6.72 (dd, J =3.6, 8.4 Hz, 1H), 4.73 (d, J =4.8 Hz, 2H), 4.56 (t, J =8.8 Hz, 2H), 3.37 - 3.29 (m, 2H), 3.26 (s, 3H), 2.28 (s, 3H).

Reference： [1]Current Patent Assignee: MIRATI THERAPEUTICS, INC. - WO2019/152419, 2019, A1 Location in patent: Paragraph 0427-042
[2]Current Patent Assignee: MIRATI THERAPEUTICS, INC. - WO2020/247475, 2020, A1 Location in patent: Paragraph 0436-0437

12
[ 1011459-26-9 ]
tert-butyl (1-(8-bromo-5-(((5-fluoro-2,3-dihydrobenzofuran-4-yl)methyl)amino)imidazo[1,2-c]pyrimidin-2-yl)ethyl)carbamate [ No CAS ]
tert-butyl (1-(5-(((5-fluoro-2,3-dihydrobenzofuran-4-yl)methyl)amino)-8-(2-methyl-4-(methylsulfonyl)phenyl)imidazo[1,2-c]pyrimidin-2-yl)ethyl)carbamate [ No CAS ]

Yield	Reaction Conditions	Operation in experiment
	With (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride; sodium hydrogencarbonate In 1,4-dioxane; water at 100℃; for 0.5h; Inert atmosphere;	34.A 2-(1-aminoethyl)-N-((5-fluoro-2,3-dihydrobenzofuran-4-yl)methyl)-8-(2-methyl-4-(methylsulfonyl)phenyl)imidazo[1,2-c]pyrimidin-5-amine [0454] Step A: A mixture of tert-butyl (1-(8-bromo-5-(((5-fluoro-2,3-dihydrobenzofuran-4-yl)methyl)amino)imidazo[1,2-c]pyrimidin-2-yl)ethyl)carbamate (70.0 mg, 138 mol, 1.00 eq.), 4,4,5,5-tetramethyl-2-(2-methyl-4-(methylsulfonyl)phenyl)-1,3,2-dioxaborolane (81.9 mg, 276 mol, 2.00 eq.), Pd(dppf)Cl2 (10.1 mg, 13.8 mol, 0.10 eq.) and sodium bicarbonate (34.8 mg, 415 mol, 16.1 L, 3.00 eq.) in a mixture solvent of water (0.40 mL) and dioxane (2.00 mL) was degassed and purged with nitrogen for 3 times, and then the mixture was stirred at 100 °C for 30 minutes under a nitrogen atmosphere. After completion of the reaction, the reaction mixture was evaporated to give a residue. The residue was purified by prep-TLC (SiO2, petroleum ether/ethyl acetate= 1/1) to give tert-butyl (1-(5-(((5-fluoro-2,3-dihydrobenzofuran-4-yl)methyl)amino)-8-(2-methyl-4-(methylsulfonyl)phenyl)imidazo[1,2-c]pyrimidin-2-yl)ethyl)carbamate (80.0 mg, crude) as yellow oil. LCMS [M+1]: 596.1.

Reference： [1]Current Patent Assignee: MIRATI THERAPEUTICS, INC. - WO2020/247475, 2020, A1 Location in patent: Paragraph 0454

13
[ 1011459-26-9 ]
tert-butyl (1-(8-bromo-5-(((5-fluoro-2,3-dihydrobenzofuran-4-yl)methyl)amino)imidazo[1,2-c]pyrimidin-2-yl)ethyl)carbamate [ No CAS ]
2-(1-aminoethyl)-N-((5-fluoro-2,3-dihydrobenzofuran-4-yl)methyl)-8-(2-methyl-4-(methylsulfonyl)phenyl)imidazo[1,2-c]pyrimidin-5-amine [ No CAS ]

Yield	Reaction Conditions	Operation in experiment
	Multi-step reaction with 2 steps 1: (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride; sodium hydrogencarbonate / water; 1,4-dioxane / 0.5 h / 100 °C / Inert atmosphere 2: trifluoroacetic acid / dichloromethane / 0.5 h / 25 °C

Reference： [1]Current Patent Assignee: MIRATI THERAPEUTICS, INC. - WO2020/247475, 2020, A1

14
[ 1011459-26-9 ]
ethyl 8-bromo-5-(((5-fluoro-2,3-dihydrobenzofuran-4-yl)methyl)amino)imidazo[1,2-c]pyrimidine-2-carboxylate [ No CAS ]
ethyl 5-(((5-fluoro-2,3-dihydrobenzofuran-4-yl)methyl)amino)-8-(2-methyl-4-(methylsulfonyl)phenyl)imidazo[1,2-c]pyrimidine-2-carboxylate [ No CAS ]

Yield	Reaction Conditions	Operation in experiment
100 mg	With (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride; sodium hydrogencarbonate In 1,4-dioxane; water at 95℃; for 1h; Inert atmosphere;	2 (5-(((5-fluoro-2,3-dihydrobenzofuran-4-yl)methyl)amino)-8-(2-methyl-4-(methylsulfonyl)phenyl)imidazo[1,2-c]pyrimidin-2-yl)methanol [0396] A mixture of ethyl 8-bromo-5-[(5-fluoro-2,3-dihydrobenzofuran -4-yl)methylamino]imidazo[1,2-c]pyrimidine-2-carboxylate (120 mg, 275 mol, 1.00 eq.), 4,4,5,5-tetramethyl-2-(2-methyl-4-(methylsulfonyl)phenyl)-1,3,2-dioxaborolane (100 mg, 332 mol, 1.21 eq.), Pd(dppf)Cl2 (20.2 mg, 27.6 mol, 0.10 eq.) and sodium bicarbonate (69.5 mg, 827 mol, 32.2 L, 3.00 eq.) in dioxane (2.00 mL), water (0.20 mL) was degassed and purged with nitrogen for 3 times, and then the mixture was stirred at 95 °C for 1hour under nitrogen atmosphere. The reaction mixture was filtered and concentrated under reduced pressure to give a residue. The residue was triturated with methanol (3.00 mL), the suspension was filtered, the filter cake was collected and dried in vacuum to give ethyl 5-(((5-fluoro-2,3-dihydrobenzofuran-4-yl)methyl)amino)-8-(2-methyl-4- (methylsulfonyl)phenyl)imidazo[1,2-c]pyrimidine-2-carboxylate (100 mg,, 68.4 % yield, 99.0% purity) as a white solid. LCMS [M+1]: 525.0.

Reference： [1]Current Patent Assignee: MIRATI THERAPEUTICS, INC. - WO2020/247475, 2020, A1 Location in patent: Paragraph 0396

15
[ 1011459-26-9 ]
ethyl 8-bromo-5-(((5-fluoro-2,3-dihydrobenzofuran-4-yl)methyl)amino)imidazo[1,2-c]pyrimidine-2-carboxylate [ No CAS ]
(5-(((5-fluoro-2,3-dihydrobenzofuran-4-yl)methyl)amino)-8-(2-methyl-4-(methylsulfonyl)phenyl)imidazo[1,2-c]pyrimidin-2-yl)methanol [ No CAS ]

Yield	Reaction Conditions	Operation in experiment
	Multi-step reaction with 2 steps 1: (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride; sodium hydrogencarbonate / water; 1,4-dioxane / 1 h / 95 °C / Inert atmosphere 2: lithium aluminium tetrahydride / tetrahydrofuran / 1 h / 0 - 25 °C

Reference： [1]Current Patent Assignee: MIRATI THERAPEUTICS, INC. - WO2020/247475, 2020, A1

16
[ 1011459-26-9 ]
8-bromo-5-(((5-fluoro-2,3-dihydrobenzofuran-4-yl)methyl)amino)imidazo[1,2-c]pyrimidine-2-carbonitrile [ No CAS ]
2-(aminomethyl)-N-((5-fluoro-2,3-dihydrobenzofuran-4-yl)methyl)-8-(2-methyl-4-(methylsulfonyl)phenyl)imidazo[1,2-c]pyrimidin-5-amine hydrochloride [ No CAS ]

Yield	Reaction Conditions	Operation in experiment
	Multi-step reaction with 2 steps 1: dichloro(1,1'-bis(diphenylphosphanyl)ferrocene)palladium(II)*CH₂Cl₂; sodium hydrogencarbonate / water; 1,4-dioxane / 1 h / 95 °C / Inert atmosphere 2: hydrogen; ammonium hydroxide / methanol / 12 h / 25 °C / 775.74 Torr

Reference： [1]Current Patent Assignee: MIRATI THERAPEUTICS, INC. - WO2020/247475, 2020, A1

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{[ item.p_purity ]}	{[ item.pr_size ]}	{[ getRatePrice(item.pr_usd, 1,1) ]} {[ getRatePrice(item.pr_usd,item.pr_rate,item.mem_rate) ]}	{[ getRatePrice(item.pr_usd, 1,1) ]}	{[ getRatePrice(item.pr_usd,item.pr_rate,item.mem_rate) ]} {[ getRatePrice(item.pr_usd,1,item.mem_rate) ]}	{[ item.pr_usastock ]}	Inquiry -	{[ item.pr_chinastock ]}	Inquiry -

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H413	May cause long-lasting harmful effects to aquatic life
H420	Harms public health and the environment by destroying ozone in the upper atmosphere

[ CAS No. 1011459-26-9 ]

Quality Control of [ 1011459-26-9 ]

Related Doc. of [ 1011459-26-9 ]

Product Details of [ 1011459-26-9 ]

Safety of [ 1011459-26-9 ]

Application In Synthesis of [ 1011459-26-9 ]

[ 1011459-26-9 ] Synthesis Path-Downstream 1~16

Related Functional Groups of [ 1011459-26-9 ]

Organoboron

Aryls

Esters

Sulfones

Precautionary Statements-General

Prevention

Response

Storage

Disposal

Physical hazards

Health hazards

Environmental hazards

Inquiry

Related Functional Groups of
[ 1011459-26-9 ]