Water → HCID 178423421, compound

Participants

Reaction Steps

To a 604 mg of N,N-diisopropylethylamine in 4 ml of methylene chloride, 10 mg of 4-dimethylaminopyridine and 613 mg of benzo[b]thiophene-2-carbonylchloride were added, and the mixture was stirred for 60 minutes. To the mixture was added dropwise a solution of 800 mg of N-{(1R,2S)-2-[(2-amino-6-methylquinazolin-4-yl)amino]cyclohexyl}-N′,N″-bis(tert-butoxycarbonyl)guanidine obtained in Reference Example 1 in 5 ml of methylene chloride, followed by stirring at room temperature for 15 hours. The reaction solution was mixed with water, extracted with methylene chloride and then dried. The solvent was distilled off and the residue was purified by silica gel column chromatography (chloroform:methanol=30:1) to obtain 890 mg of the desirable compound.

Provenance & Evidence