【药物名称】OPB-3206
化学结构式(Chemical Structure):
参考文献No.24961
标题:Carbostyril derivs. as matrix metalloproteinases inhibitors
作者:Sakamoto, M.; Imaoka, T.; Motoyama, M.; Yamamoto, Y.; Takasu, H. (Otsuka Pharmaceutical Co., Ltd.)
来源:EP 0641323; JP 1995157470; WO 9421612
合成路线图解说明:

The protection of the amino group of 3(S)-amino-1-hydroxy-1,2,3,4-tetrahydroquinolin-2-one (I) with tert-butoxycarbonyl anhydride gives the carbamate (II), which is methylated with NaH and methyl iodide in DMF yielding the N-methoxy derivative (III). The deprotection of (III) with TFA and its condensation with 2(R)-isobutylsuccinic acid 4-tert-butyl monoester (IV) by means of DCC and HOBT in DMF affords the succinamic ester (V), which is hydrolyzed with TFA to give the succinamic acid (VI). The reaction of (VI) with O-benzylhydroxylamine by means of HOBT in DMF yields the benzyl hydroxamate (VII), which is finally debenzylated by hydrogenation with H2 over Pd/C in ethanol.

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