Hydrochloric Acid → HCID 178478809, compound

Participants

Reaction Steps

Pyrazole-1-carboxamidine hydrochloride (284 mg) was added to a mixed solution of N-(1H-pyrazolo[3,4-b]pyridin-4-yl)-4-aminomethylbenzamide dihydrochloride (330 mg) and diisopropylethylamine (500 mg) in methanol (5 ml)-dimethylformamide (5 ml), and the mixture was stirred in a stream of nitrogen at room temperature for 8 hours. After the reaction, the reaction mixture was concentrated under reduced pressure. The obtained residue was purified by silica gel column chromatography (chloroform:methanol=3:1) to give white crystals. The crystals were converted to hydrochloride thereof with 15% hydrochloric acid-methanol, and the hydrochloride was recrystallized from methanol-ether to give 205 mg of N-(1H-pyrazolo[3,4-b]pyridin-4-yl)-4-guanidinomethylbenzamide dihydrochloride monohydrate having a melting point of 250-254° C. (dec.)

Provenance & Evidence