2-氟-5-甲酰基苯甲酸的合成及工艺优化

Synthesis and Process Optimization of 2-Fluoro-5-formylbenzoic Acid

2-氟-5-甲酰基苯甲酸是合成奥拉帕尼等的关键中间体。以2-氟-5-甲酰基苯腈为原料,经乙二醇保护醛基、氰基水解、脱保护三步得到目标化合物2-氟-5-甲酰基苯甲酸,并对各步反应条件进行了优化,三步反应平均收率77.8%。目标化合物2-氟-5-甲酰基苯甲酸经1 H NMR和MS表证。

2-Fluoro-5-formylbenzoic acid,an important intermediate of olperapib,was synthesized by using2-fluoro-5-formylbenzonitrile as starting material via reacting with ethylene glycol to protect the aldehyde group,followed by cyanide hydrolyzation and deprotection with an overall yield of 77.8%.The reaction conditions of all steps were optimized.The chemical structure of product was confirmed by 1 H NMR and MS.