Ao Chen, Ziqian Li, Minghai Li, Keke Liu, Weimin Li and Chen Tan* Pages 802 - 806 ( 5 )
4-Methylenepiperidine hydrochloride 1 is a key intermediate for synthesis of the novel antifungal drug efinaconazole 2. In this work, a simple and robust process has been developed to synthesize 4-methylenepiperidine hydrochloride 1, with a high overall yield of 99.1% at a high purity of 99.7% in a large-scale. Moreover, this synthetic process avoided the uses of organolithium reagent and column chromatography process which are not desirable for industrial production.
4-methylenepiperidine hydrochloride, efinaconazole, drug, intermediate, synthetic process, large-scale.
Shanghai Pharma Group Changzhou Kony Pharmaceutical Co., Ltd., Changzhou, 213105, Undergraduate Department, University of Chinese Academy of Sciences, Beijing, 100049, Shanghai Pharma Group Changzhou Kony Pharmaceutical Co., Ltd., Changzhou, 213105, Shanghai Pharma Group Changzhou Kony Pharmaceutical Co., Ltd., Changzhou, 213105, School of Petrochemical Engineering, Changzhou University, Changzhou 213164, School of Chemistry and Materials Science, University of Science and Technology of China, Hefei, 230026