新产品编号:1807153

Chemical Name: (3bS,4aR)-6-[3-[4-[4-(Acetylamino)-1-methyl-1H-imidazol-2-ylcarboxamido]-1-methyl-1H-pyrrol-2-yl]-2(E)-propenoyl]-2-methyl-8-oxo-1,4,4a,5,6,8-hexahydrocyclopropa[c]pyrrolo[3,2-e]indole-3-carboxylic acid methyl ester
项目整合开发状态: Biological Testing
项目研究机构: Kyoto University (Originator), Tokyo Medical and Dental University (Originator)
合成路线:The pyrrolecarboxylic acid derivative (I) was treated with BOP reagent,and the resulting hydroxybenzotriazolyl ester was reduced in situ with NaBH4 to furnish alcohol (II).Oxidation of (II) by means of activated MnO2 produced aldehyde (III).Wadsworth-Emmons reaction of aldehyde (III) with triethylphosphonoacetate gave rise to the unsaturated ester (IV).After basic hydrolysis of the ester group of (IV),the resultant carboxylic acid (V) was activated as the imidazolide (VI) upon treatment with carbonyldiimidazole.This was finally coupled with the segment A of DU86 (VII) in the presence of NaH in DMF at low temperature to yield the target amide.