Patamostat mesylate, E-3123-药物合成数据库

【药物名称】Patamostat mesylate, E-3123

化学结构式(Chemical Structure):

参考文献No.	6560
标题:	Guanidinobenzoic ester deriv., a process for preparing same and pharmaceutical compsns. containing same
作者:	Hishinuma, I.; Kawashima, H.; Kawata, T.; Miyamoto, K.; Miyazawa, S.; Nagakawa, J.; Nagaoka, J.; Nagaoka, N.; Shimomura, N.; Souda, S.; Ueda, N.; Wakabayashi, T.; Yamanaka, T. (Eisai Co., Ltd.)
来源:	EP 0229370; JP 1987155253; JP 1994298730; US 4801603; US 5075335

合成路线图解说明: The alkylation of succinimide (I) with 1,2-dibromoethane (II) by means of K2CO3 in refluxing butanone gives N-(2-bromoethyl)succinimide (III), which is condensed with 4-hydroxythiophenol (IV) by means of K2CO3 in refluxing ethanol to afford 4-hydroxyphenyl 2-succinimidoethyl sulfide (V). Finally, this compound is esterified with 4-guanidinobenzoyl chloride in pyridine, and treated with methanesulfonic acid in methanol.

参考文献No.	63022
标题:	E-3123
作者:	Prous, J.; Casta馿r, J.
来源:	Drugs Fut 1988,13(7),613

合成路线图解说明: The alkylation of succinimide (I) with 1,2-dibromoethane (II) by means of K2CO3 in refluxing butanone gives N-(2-bromoethyl)succinimide (III), which is condensed with 4-hydroxythiophenol (IV) by means of K2CO3 in refluxing ethanol to afford 4-hydroxyphenyl 2-succinimidoethyl sulfide (V). Finally, this compound is esterified with 4-guanidinobenzoyl chloride in pyridine, and treated with methanesulfonic acid in methanol.