新产品编号:1380013

Chemical Name: 3-[4-(3-Cyclopentyloxy-4-methoxyphenyl)-2-oxopyrrolidin-1-yl]-5-(3-methoxybenzyloxy)benzoic acid
项目整合开发状态: Preclinical
项目研究机构: Novartis (Originator)
合成路线:Methyl 5-hydroxy-3-iodobenzoate (I) was protected as the benzyl ether (II).Subsequent coupling of (II) with rolipram (III) in the presence of K2CO3 and copper catalyst afforded the N-aryl derivative (IV),which was debenzylated by hydrogenation over Pd/C.The resulting phenol (V) was alkylated with 3-methoxybenzyl chloride (VI) to provide ether (VII).Further basic hydrolysis of the methyl ester of (VII) yielded the corresponding carboxylic acid (VIII).This was finally coupled with N,N-dimethylhydrazine by means of EDC and HOBt to furnish the target hydrazide.

合成路线:Methyl 5-hydroxy-3-iodobenzoate (I) was protected as the benzyl ether (II).Subsequent coupling of (II) with rolipram (III) in the presence of K2CO3 and copper catalyst afforded the N-aryl derivative (IV),which was debenzylated by hydrogenation over Pd/C.The resulting phenol (V) was alkylated with 3-methoxybenzyl chloride (VI) to provide ether (VII).Finally,basic hydrolysis of the methyl ester of (VII) furnished the corresponding carboxylic acid.