D-43787

2-甲基-2-丙基2-({2-[(6-{[(苄氧基)羰基]氨基}-1-甲氧基-1-氧代-2-己烷基)氨基甲酰]-2,3-二氢-1H-吲哚-1-基}羰基)-1-吲哚啉羧酸酯Chemical Name: Nepsilon-(Benzyloxycarbonyl)-Nalpha-[1-[1-(tert-butoxycarbonyl)indolin-2(S)-ylcarbonyl]indolin-2(S)-ylcarbonyl]-L-lysine methyl ester
CAS No. 198016-44-3 (diastereomer)
项目整合开发状态: Preclinical
项目研究机构: Asta Medica (Originator), Ivax (Codevelopment)
合成路线:Indoline-2-carboxylic acid (I) is converted into the N-Boc derivative (II) by treatment with Boc2O.Subsequent coupling of (II) with methyl indoline-2-carboxylate (III) by using 2-chloro-1-methylpyridinium iodide (CMPI) provides amide (IV).Hydrolysis of the methyl ester function of (IV) employing LiOH leads to carboxylic acid (V).This is then coupled to N-epsilon-(benzyloxycarbonyl)-lysine methyl ester (VI) in the presence of CMPI to furnish the title compound.