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With caesium carbonate;tris-(dibenzylideneacetone)dipalladium(0); 4,5-bis(diphenylphos4,5-bis(diphenylphosphino)-9,9-dimethylxanthenephino)-9,9-dimethylxanthene; In 1,4-dioxane; at 90℃; for 14h;
Benzo[1 ,2,5]thiadiazol-5-yl-(8-chloro-[1 ,2,4]triazolo[1 ,5-a]pyrazin-2-yl)-amine ("BIO")100 mg (0.6 mmol) of 8-pyridin-3-yl-[1 ,2,4]triazolo[1 ,5-a]pyrazin-2-ylamine, mg (0.9 mmol) 5-bromo-2,1 ,3-benzothiadiazole, 68 mg (0.1 mmol) 9,9- dimethyl-4,5-bis(diphenylphosphino)xanthene , 578 mg (1.8 mmol) cesium carbonate and 34 mg bis(dibenzylideneacetone)palladium are dissolved in 1 ml dioxane and stirred at 90 C for 14 h. HPLC and LC-MS analysis show formation of the product (LCMS (method C): mass found (M+H+, 303), HPLC (method D) Rt (min): 3.07.
With potassium carbonate; In N,N-dimethyl-formamide; at 180℃;Microwave irradiation;
General Procedure for nucleophilic aromatic Substitution 3To a microwave vial stir bar is added 1 eq. of triazolopyrazine, 1.1 eq. of the corresponding amine and potassium carbonate (2 eq). N,N-dimethylformamide (3 mL / mmol) is added and the suspension heated in the microwave at 180C. The reaction is monitored by HPLC. Upon completion, the mixtured is diluted with ethylacetate, filtered over Celite and concentrated. The residue is purified via column chromatography or preparative HPLC.(3,5-Dimethoxy-phenyl)-[8-(2-phenyl-pyrrolidin-1-yl)-[1,2,4]triazolo[1 ,5- a]pyrazin-2- l]-amine ("D19")Step 1 :The reaction is performed using general procedure 3 and rac-2-phenyl- pyrrolidine as coupling partner.
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