合成路线图解说明: 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. |