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Type
HazMat fee for 500 gram (Estimated)
Excepted Quantity
USD 0.00
Limited Quantity
USD 15-60
Inaccessible (Haz class 6.1), Domestic
USD 80+
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Structure of 121-60-8 * Storage: {[proInfo.prStorage]}
* 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.
Reference：
[1] European Journal of Medicinal Chemistry, 2017, vol. 136, p. 63 - 73
8
[ 121-60-8 ]
[ 68-35-9 ]
Reference：
[1] Dansk Tidsskrift for Farmaci, 1942, vol. 16, p. 141,150
[2] Patent: CH230861, 1938, ,
[3] Journal of the American Chemical Society, 1940, vol. 62, p. 2002,2003[4] Journal of the American Chemical Society, 1942, vol. 64, p. 567,568
[5] Patent: WO2017/156181, 2017, A1,
9
[ 108-52-1 ]
[ 121-60-8 ]
[ 127-79-7 ]
Reference：
[1] European Journal of Medicinal Chemistry, 2017, vol. 136, p. 63 - 73
10
[ 121-60-8 ]
[ 127-79-7 ]
Reference：
[1] Journal of the American Chemical Society, 1942, vol. 64, p. 2340
[2] Patent: CH230863, 1938, ,
[3] Journal of the American Chemical Society, 1941, vol. 63, p. 3028
[4] Journal of the American Chemical Society, 1940, vol. 62, p. 2002,2003[5] Journal of the American Chemical Society, 1942, vol. 64, p. 567,568
[6] Recueil des Travaux Chimiques des Pays-Bas, 1942, vol. 61, p. 627,666,667
[7] J.Chin.chem.Soc., 1947, vol. 15, p. 138,145
11
[ 121-60-8 ]
[ 144-82-1 ]
Reference：
[1] Recueil des Travaux Chimiques des Pays-Bas, 1943, vol. 62, p. 207
[2] Archiv der Pharmazie (Weinheim, Germany), 1951, vol. 284, p. 53,57
[3] Bioorganic and Medicinal Chemistry, 2011, vol. 19, # 6, p. 2046 - 2054
[4] Patent: WO2009/129267, 2009, A2,
12
[ 108-33-8 ]
[ 121-60-8 ]
[ 144-82-1 ]
Reference：
[1] Patent: CH230860, 1938, ,
[2] Patent: DE957841, 1957, ,
[3] Proceedings - Indian Academy of Sciences, Section A, 1941, # 13, p. 386,387
13
[ 2302-95-6 ]
[ 121-60-8 ]
[ 144-82-1 ]
Reference：
[1] Patent: US2447702, 1942, ,
14
[ 121-60-8 ]
[ 57-68-1 ]
Reference：
[1] Journal of the American Chemical Society, 1941, vol. 63, p. 2188
[2] Patent: CH230865, 1938, ,
Reference：
[1] Yakugaku Zasshi, 1951, vol. 71, p. 1356,1358[2] Chem.Abstr., 1952, p. 8036
[3] Yakugaku Zasshi, 1951, vol. 71, p. 1356,1358[4] Chem.Abstr., 1952, p. 8036
[5] Antimicrobial Agents and Chemotherapy, 2014, vol. 58, # 5, p. 2968 - 2971
17
[ 7252-84-8 ]
[ 121-60-8 ]
[ 80-35-3 ]
Reference：
[1] European Journal of Medicinal Chemistry, 2017, vol. 136, p. 63 - 73
18
[ 1072-67-9 ]
[ 121-60-8 ]
[ 21312-10-7 ]
Yield
Reaction Conditions
Operation in experiment
59%
at 20℃; for 12 h;
A mixture of 4-acetamidobenzene-1-sulfonyl chloride (4.27 mmol), 5-methylisoxazol-3-amine (4.49 mmol) and DMAP (0.21 mmol) in anhydrous pyridine (10 mL) was stirred at room temperature for 12 h. After completion of reaction, solvent was evaporated to dryness and diluted with water and extracted with ethyl acetate. The combined organic layers were washed with water and 1 M aqueous HCl, dried over anhydrous Na2SO4, filtered, and concentrated under vacuum. The solid residue obtained was purified with flash column chromatography using heptanes to EtOAc (50-100percent) gradient elution to afford the compound 2. 4.2.1 N-(4-(N-(5-Methylisoxazol-3-yl)sulfamoyl)phenyl)acetamide (2) Yield: 59percent; ESIMS m/z calcd for C12H13N3O4S [M + H]+, 296.07; found 296.06; 1H NMR (400 MHz, (CD3)2SO): δ 11.30 (bs, 1H), 10.35 (bs, 1H), 7.79-7.73 (m, 4H), 6.12 (s, 1H), 2.29 (s, 3H), 2.07 (s, 3H). 13C (100 MHz, (CD3)2SO): δ 170.71, 169.57, 158.07, 144.01, 133.36, 128.50, 119.15, 95.84, 24.57, 12.48.
Reference：
[1] ACS Medicinal Chemistry Letters, 2014, vol. 5, # 1, p. 12 - 17
[2] European Journal of Medicinal Chemistry, 2015, vol. 101, p. 595 - 603
[3] Shionogi Kenkyusho Nenpo, 1957, # 7, p. 301,304[4] Chem.Abstr., 1957, p. 17889
[5] Patent: US2888455, 1957, ,
[6] Crystal Growth and Design, 2013, vol. 13, # 9, p. 4002 - 4016
[7] Patent: CN105884705, 2016, A, . Location in patent: Paragraph 0013; 0016; 0021; 0026; 0031
19
[ 121-60-8 ]
[ 122-11-2 ]
Reference：
[1] Monatshefte fuer Chemie, 1956, vol. 87, p. 136,142
20
[ 4774-10-1 ]
[ 121-60-8 ]
[ 152-47-6 ]
Reference：
[1] Crystal Growth and Design, 2013, vol. 13, # 9, p. 4002 - 4016
Reference：
[1] Journal of Organic Chemistry, 1956, vol. 21, p. 520
24
[ 121-60-8 ]
[ 2360-19-2 ]
Reference：
[1] Journal of the Chemical Society, 1939, p. 608
25
[ 100-01-6 ]
[ 121-60-8 ]
[ 122-16-7 ]
Yield
Reaction Conditions
Operation in experiment
40%
at 20℃;
General procedure: To a solution of the aniline 1a-l (1 eq) in pyridine (1.6 mL/mmol) was added4-acetamidobenzenesulfonyl chloride (1.1 eq), the mixture was stirred at room temperature overnight, quenched with water and extracted three times with EtOAc. The combinedorganic layers were washed three times with 0.5 N HCl, three times with water and oncewith brine. The organic phase was then dried with anhydrous MgSO4, filtered, andconcentrated to give the title compound as a solid.
Reference：
[1] Bioorganic and Medicinal Chemistry Letters, 2017, vol. 27, # 18, p. 4426 - 4430
[2] Patent: US2282769, 1939, ,
[3] Journal of the American Chemical Society, 1939, vol. 61, p. 613,616
[4] DRP/DRBP Org.Chem.,
[5] Canadian Journal of Research, Section B: Chemical Sciences, 1942, vol. 20, p. 5,7, 9
[6] Journal of the American Chemical Society, 1938, vol. 60, p. 1553
[7] Journal of Organic Chemistry, 1947, vol. 12, p. 275,278, 280
[8] Phosphorus, Sulfur and Silicon and the Related Elements, 2009, vol. 184, # 1, p. 92 - 102
[9] Bioorganic and Medicinal Chemistry Letters, 2009, vol. 19, # 16, p. 4574 - 4578
[10] Crystal Growth and Design, 2011, vol. 11, # 4, p. 1067 - 1081
[11] Journal of Enzyme Inhibition and Medicinal Chemistry, 2012, vol. 27, # 5, p. 628 - 640
[12] DRP/DRBP Org.Chem.,
[13] Patent: US2282769, 1939, ,
26
[ 121-60-8 ]
[ 587850-67-7 ]
Reference：
[1] Journal of the Indian Chemical Society, 1941, vol. 18, p. 316,319
General procedure: A suspension of 5-aminouracil 1 (1 mmol) in dry pyridine (7.5 mL) was cooled to 0 C and the appropriate sulfonyl chloride (1 mmol) was added. The reaction mixture was stirred at room temperature until the TLC showed the reaction was completed (1.5-20 h). The solvent was removed under reduced pressure and the crude product was recrystallized from methanol or aqueous methanol to afford the product.
With triethylamine; In N,N-dimethyl-formamide; at 15℃; for 14h;Large scale;
(1) In a 2000 L dry reactor, 4-amino-2,6-dimethoxypyrimidine (456 kg)1200 kg of N, N-dimethylformamide (DMF), 303 kg of triethylamine,In stirring under the inputAcetaminobenzene sulfonyl chloride (ASC) 701kg,Internal temperature control at 15 , 2h plus finished. After adding, insulation 12h.After the tracing reaction is complete, DMF is recovered in high vacuum and excess triethylamine (applied).The autoclave was added 1200kg of ethyl acetate, heated to 65 C, filtered while hot,The filter cake is triethylamine hydrochloride. The filtrate was cooled to 0 C and centrifuged to obtain a wet product 1;Centrifuged mother liquor was concentrated to 1/4 of the volume, then cooled to 0 C and centrifuged to obtain wet product 2.The mixed wet product 1 and the wet product 2 are dried to obtain a condensation product4-p-acetamidobenzenesulfonamido-2,6-dimethoxypyrimidine 1024.59kg, yield 99%Content of more than 98.5%.Ethyl acetate applied, triethylamine hydrochloride for co-processing.
1-(3,5-dichloropyridin-4-yl)-4-(3-methylphenyl)sulfonyl-1,4-diazepane[ No CAS ]
1-(3,5-dichloropyridin-4-yl)-4-(4-methylphenyl)sulfonyl-1,4-diazepane[ No CAS ]
1-(3,5-dichloropyridin-4-yl)-4-(2-methylphenyl)sulfonyl-1,4-diazepane[ No CAS ]
1-(3,5-dichloropyridin-4-yl)-4-(3-methoxyphenyl)sulfonyl-1,4-diazepane[ No CAS ]
1-(3,5-dichloropyridin-4-yl)-4-(4-methoxyphenyl)sulfonyl-1,4-diazepane[ No CAS ]
1-(3,5-dichloropyridin-4-yl)-4-(2-methoxyphenyl)sulfonyl-1,4-diazepane[ No CAS ]
1-(3,5-dichloropyridin-4-yl)-4-(4-propan-2-ylphenyl)sulfonyl-1,4-diazepane[ No CAS ]
1-(3-chlorophenyl)sulfonyl-4-(3,5-dichloropyridin-4-yl)-1,4-diazepane[ No CAS ]
1-(3,5-dichloropyridin-4-yl)-4-(4-fluorophenyl)sulfonyl-1,4-diazepane[ No CAS ]
1-(2-chlorophenyl)sulfonyl-4-(3,5-dichloropyridin-4-yl)-1,4-diazepane[ No CAS ]
2-[[4-(3,5-dichloropyridin-4-yl)-1,4-diazepan-1-yl]sulfonyl]benzonitrile[ No CAS ]
1-[4-[[4-(3,5-dichloropyridin-4-yl)-1,4-diazepan-1-yl]sulfonyl]phenyl]ethanone[ No CAS ]
1-(2,4-dichlorophenyl)sulfonyl-4-(3,5-dichloropyridin-4-yl)-1,4-diazepane[ No CAS ]
1-(3,5-dichloropyridin-4-yl)-4-naphthalen-1-ylsulfonyl-1,4-diazepane[ No CAS ]
1-(3,5-dichloropyridin-4-yl)-4-naphthalen-2-ylsulfonyl-1,4-diazepane[ No CAS ]
1-(3,5-dichloropyridin-4-yl)-4-[2-(trifluoromethyl)phenyl]sulfonyl-1,4-diazepane[ No CAS ]
1-(3,5-dichloropyridin-4-yl)-4-[4-(trifluoromethyl)phenyl]sulfonyl-1,4-diazepane[ No CAS ]
N-[4-[[4-(3,5-dichloropyridin-4-yl)-1,4-diazepan-1-yl]sulfonyl]phenyl]acetamide[ No CAS ]
1-(3,5-dichloropyridin-4-yl)-4-[3-(trifluoromethyl)phenyl]sulfonyl-1,4-diazepane[ No CAS ]
Yield
Reaction Conditions
Operation in experiment
With N-ethyl-N,N-diisopropylamine; In dichloromethane; at 20℃;Combinatorial reaction / High throughput screening (HTS);
Examples 1-19; General Method:; A solution of l-(3,5-dichloropyridin-4-yl)-l,4-diazepane (100 mg, 0.41 mmol) in DCM (1 ml) was added to the appropriate sulfonyl chloride (0.41 mmol) under a nitrogen atomosphere. DIPEA (0.22 ml, 1.22 mmol) was then added and the mixture stirred overnight at ambient temperature. The reaction mixtures were washed with water and the products isolated by <n="24"/>flash column chromatography (Combi-Flash Optix 10 on a 12g silica cartridge, eluting with a 1:1 mixture of EtOAc and isohexane) to give colourless solids.; The following compounds were synthesised as a multiparallel array:
With hydrogenchloride; calcium carbonate; In ice-water; water;
EXAMPLE 94 730 ml of water and 159 g of Na2 SO3 (95percent strength by weight) were introduced first. 530 g of 4-acetylaminobenzenesulfonyl chloride were then added a little at a time with stirring at 70° C., while the pH was maintained at about 9 with 95 ml of 50percent strength by weight sodium hydroxide solution. After 3 hours of subsequent stirring at 70° C., insolubles were filtered off, 250 g of ice were added at 30° C., and 375 ml of 17percent strength by weight hydrochloric acid were added with stirring at pH 1.0 to bring down a precipitate, while the temperature was maintained at <=10° C. The resulting suspension was filtered with suction after 1.5 hours and the filter residue was washed with 1.5 1 of ice-water. The filter material was then suspended in 400 ml of ice-water and dissolved at about 15° C. with 74 ml of 30percent strength by weight sodium hydroxide solution at pH 9.0. This gave 782 ml of a clear solution containing 185 g of the sodium salt of 4-acetylaminobenzenesulfinic acid. 654 ml of this solution (corresponding to 154.7 g of the sodium salt of 4-acetylaminobenzenesulfinic acid) were introduced first, and 365 g of 50percent strength by weight 2-nitrochlorobenzene-4-sulfonic acid were added with stirring at pH 6.2. The pH was then adjusted to 7.0 with a few drops of sodium hydroxide solution. 9 g of CaCO3 and 0.35 g of copper powder were added, and the mixture was stirred at 100° C. for 20 hours and then filtered hot. The resulting solution was admixed with 180 ml of 17percent strength by weight hydrochloric acid and refluxed for 4 hours. The suspension obtained was then filtered with suction at room temperature, and the filter residue was washed with 2 1 of ice-water and dried at 70° C. under reduced pressure. Yield: 250 g of 4-amino-2'-nitro-4'-sulfodiphenyl sulfone of the formula STR179
General procedure: To a solution of p-acetamidobenzenesulfonyl chloride (275 mg, 1.18 mmol) in pyridine (5 mL) was added ethyl 2-(5-amino-1,3,4-thiadiazol-2-yl)acetate (200 mg, 1.07 mmol). The reaction mixture was stirred at rt for 4.5 h, then 2 M HCl (10 mL) was added and the mixture extracted with EtOAc (3 ' 50 mL). The organic extracts were washed with water (20 mL), brine (20 mL), dried over anhydrous Na2SO4, filtered, and concentrated in vacuo. The residue was subjected to chromatography on silica gel (70-230 mesh) eluted with CH2Cl2:MeOH 19:1, affording the product 13 (312 mg, 0.81 mmol, 76percent yield),
73%
With pyridine; at 20℃; for 4.5h;
To a solution of /?-acetamidobenzenesulfonyl chloride (1.98 g, 8.47 mmol) in pyridine (20 rnL) was added ethyl 5-amino-l,3,4-thiadiazole-2-carboxylate (1.2 g, 7.06 mmol). The reaction mixture was stirred at room temperature for 4.5 h, than 2 M HCl (50 mL) was added to quench the reaction. The mixture was extracted with ethyl acetate (3 x 60 mL). The organic extracts were washed with water (50 mL), brine (50 mL), dried over Na2SO4, filtered, and concentrated. The residue was purified by chromatography on silica gel (70-230 mesh) eluted with CH2Cl2 methanol 19:1 to give the product as a solid, mp 201-202 0C, in 73percent yield (1.91 g, 5.15 mmol); 1H NMR (300 MHz, DMSO-^) delta 1.29 (t, 3H, J = 6.9 Hz), 2.08 (s, 3H), 4.37 (q, 2H, J = 7.8 Hz), 7.74 (m, 4H), 10.32 (s, IH); 13C NMR (75 MHz, OMSO-d6) delta 13.9, 14.0, 24.1, 62.9, 118.6, 127.1, 134.9, 143.2, 147.2, 157.5, 167.6, 169.0; MS (LCQ, ESI+) Calcd for Ci3Hi5N4O5S2 371.0, found 371.0 (M+H)+; HRMS (ESI+, m/z) Calcd for Ci3Hi5N4O5S2 371.0484, found 371.0472 (M+H)+.
(S)-N-(4-(N-(2-oxotetrahydrofuran-3-yl)sulfamoyl)phenyl)acetamide[ No CAS ]
Yield
Reaction Conditions
Operation in experiment
67%
With triethylamine; In ethanol; at 0 - 20℃;
<strong>[6305-38-0]L-homoserine lactone hydrobromide</strong> 2 (10.9 g, 60 mmol)and triethylamine (25.5 mL, 120 mmol) were dissolved inethanol (120 mL). 4-acetylaminobenzenesulfonyl chloride(16.8 g, 72 mmol) was added at 0 C in a portion-wisemanner. The resulting mixture was stirred overnight atambient temperature. The next day, the reaction solutionwas concentrated to 1/3 volume and poured into ice-coldwater (200 mL) with vigorous stirring for 1 h. Then thewhite solid precipitate was collected by filtration. The filtercake was washed with ice water and dried under vacuumbefore being recrystallized from ethaol to give white solid 3.(12 g, 67%); mp 174-176 C; 1H-NMR (400 Hz, DMSOd6)delta: 10.33 (s, 1H), 8.16 (d, 1H, J = 8.0 Hz), 7.75 (s, 4H),4.34-4.30 (m, 1H), 4.21 (m, 1H), 4.08 (m, 1H), 2.08-2.06(m, 4H), 1.80(m, 1H); EI-MS m/z: 299.34 [M + H]+.
67%
With triethanolamine; In ethanol; at 0 - 20℃;
(s)-N-(4-(N-(2-oxotetrahydrofuran-3-yl)sulfamoyl)phenyl)acetamide 16.8g (72mmol) p-acetamidobenzene sulfonyl chloride was added in batches to 120mL ethanol solution of 10.9g (60mmol) (L)-homoserine lactone hydrobromide (Intermediate 1) and 25.5mL (120mmol) triethanolamine at 0 C. After stirring at room temperature overnight, the reactants were poured into ice water (200mL) the next day and were stirred for 1 h. The precipitated white solids were filtrated and collected, washed with ice water, dried under vacuum, and recrystallized with ethanol, to get 12g white solids (Intermediate 2), with a yield of 67%. 1H-NMR(400MHz, DMSO)deltappm:10.33 (s, 1 H), 8.16 (d, 1 H, J=8.0 Hz), 7.75 (s, 4H), 4.34-4.30 (m, 1 H), 4.21 (m, 1 H), 4.08 (m, 1 H), 2.08-2.06 (m, 4H), 1.80(m, 1 H); EI-MS (m/z): 299.34 [M+H]+ ; m.p.174-176 C.
57%
With triethylamine; In ethanol; at 0 - 20℃;
[0043] 12.3g (52mmol) p-acetamino-benzenesulfonyl chloride was added into 80ml ethanol solution containing 8.0g(43mmol) (L)-homoserine lactone hydrobromide (intermediate 1) and 8.7g (86mmol) triethylamine at 0 C in batches,and stirred at room temperature overnight, the reactant was poured into ice water (200mL), stirred strongly for 1 hours,the precipitated white solid was collected by filtration, washed with ice water and dried in vocuum, recrystallized inethanol, to get 7.47g white solid (Intermediate 2), with a yield of 57%. 1H-NMR(400MHz,DMSO)deltappm:10.33(1H,s),8.16(1H,d,J=8.0Hz),7.75(4H,m),4.34( 1 H,m),4.21(1H,m),4.08(1H,m),2.08(4H,m),1.79(1H,m);EI-MS(m/z):299.34[M+H]+;m.p. 174-176C.
With pyridine; In acetonitrile; at 0 - 20℃; for 18h;Inert atmosphere;
Step 1: Synthesis of N-{4-[(5-methoxypyrimidin-2-yl)sulfamoyl] phenyl}acetamide 20.1 [00358] To a solution of <strong>[13418-77-4]5-methoxypyrimidin-2-amine</strong> (200 mg, 1.6 mmol) in MeCN (5 ml) was added pyridine (86 mu, 1.07 mmol) and the resulting solution was cooled to 0C. A solution of 4-(acetylamino)benzenesulfonyl chloride (250 mg, 1.07 mmol) in MeCN (10ml) was added drop wise over five minutes, the resulting mixture was stirred under nitrogen at 0C then allowed to warm to rt and stirred for 18h. The solvent was removed in vacuo and the remaining solid was purified by flash column chromatography (DCM/iPrOH 99/1 to 90/10) to afford 190 mg (41%) of N-{4-[(5-methoxypyrimidin-2-yl)sulfamoyl]phenyl}acetamide 20.1 as a white powder.
42.0 g of <strong>[696-45-7]4-amino-6-methoxypyrimidine</strong> (abbreviated as 4-MP, prepared according to Chinese patent CN 102516182) was added to 126 ml of pyridine at 0 to 5°C, and 4-p-acetyl aminobenzenesulfonyl chloride (abbreviation SCL) 87.5 g. After the addition was complete, the reaction mixture was stirred at 20-30 ° C until the 4-MP remained After completion of the reaction, 450 ml of ultrapure water was added and the supernatant was removed from the reaction mixture.
N,N’-di(4-acetamidobenzenesulfonyl)-2,2'-bis(trifluoromethyl)benzidine[ No CAS ]
Yield
Reaction Conditions
Operation in experiment
28 g
With sodium carbonate; In tetrahydrofuran; at 20℃;
24 g of 2,2'-bis (trifluoromethyl) benzidine was dissolved in 170 ml of tetrahydrofuran (THF), and 38.5 g of N-acetamidobenzenesulfonyl chloride and 23.8 g of sodium carbonate were added to the reaction solution. After stirring at room temperature, And the reaction solution was filtered.The filtrate was concentrated under reduced pressure, and 240 ml of water and 15 g of 50% sodium hydroxide (NaOH) were added. The mixture was stirred for 30 minutes and then layered.The water layer was washed three times with 100 ml of ethyl acetate, acidified (pH = 4) with aqueous hydrochloric acid solution and then extracted with 700 ml of ethyl acetate.The separated organic layer was washed three times with 100 ml of water, and the separated organic layer was dried with anhydrous sodium sulfate (Na2SO4).The solid was filtered, and the filtrate was concentrated when the crystals were precipitated so as to be filtered.This was heated and dried to obtain 28 g of white crystalline N, N'-Di (4-acetamidobenzenesulfonyl) -2,2'-bis (trifluoromethyl) benzidine having an HPLC purity of 99.6%.
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