反应详情

414 mg (0.482 mmol) of 2-{4-(2-({(2-(4-chlorophenyl)-1,3-thiazol-4-yl)methyl}sulfanyl)-3,5-dicyano-6-(pyrrolidin-1-yl)pyridin-4-yl)phenoxy}ethyl N-(tert-butoxycarbonyl)-L-isoleucyl-L-alaninate were dissolved in 3 ml dichloromethane, and 4.822 ml of a 1N solution of hydrogen chloride in diethyl ether were added. After 6 hours of stirring, 2 ml of a 1N solution of hydrogen chloride in diethyl ether were added, and the mixture was stirred at room temperature for a further 24 hours. The precipitated solid was filtered off with suction, washed with diethyl ether and dried under reduced pressure. Since the reaction was still incomplete, the solid was stirred in 5 ml of a 1N solution of hydrogen chloride in diethyl ether for a further 24 h. The precipitated solid was filtered off with suction, washed with diethyl ether and dried under reduced pressure. 312 mg (81% of theory) of the target compound were obtained.

1. stirringthe mixture was stirred at room temperature for a further 24 hours
2. filtrationThe precipitated solid was filtered off with suction
3. washwashed with diethyl ether
4. customdried under reduced pressure
5. stirringthe solid was stirred in 5 ml of a 1N solution of hydrogen chloride in diethyl ether for a further 24 h
6. filtrationThe precipitated solid was filtered off with suction
7. washwashed with diethyl ether
8. customdried under reduced pressure
9. custom312 mg (81% of theory) of the target compound were obtained