Synthesis of 2-Chloronicotinic Acid Derivatives

Abstract

2-Chloronicotinic acid and its derivatives are important intermediates for the synthesis of medical antibiotics, anti-cardiovascular drugs, insecticides and herbicides, and they used in the synthesis pranoprofen and diflufenican. In this work, a rapid synthetic method for 2-morpholinonicotinic acid was established. The 2-morpholinonicotinic acid was synthesized from the commercially available dichloro-hydrochloric acid through three steps including esterification, nucleophilic substitution and hydrolysis. The structures were confirmed by MS. Furthermore, the synthetic method was optimized, and the total yield of the three steps was 93 %.