A Simple and Robust Process for Large-Scale Synthesis of 4-Methylenepiperidine Hydrochloride

Title:A Simple and Robust Process for Large-Scale Synthesis of 4-Methylenepiperidine Hydrochloride

Volume: 16 Issue: 10

Author(s): Ao Chen, Ziqian Li, Minghai Li, Keke Liu, Weimin Li and Chen Tan*

Affiliation:

• School of Chemistry and Materials Science, University of Science and Technology of China, Hefei, 230026,China

Keywords: 4-methylenepiperidine hydrochloride, efinaconazole, drug, intermediate, synthetic process, large-scale.

Abstract: 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.

Cite this article as:

Chen Ao , Li Ziqian , Li Minghai , Liu Keke , Li Weimin and Tan Chen *, A Simple and Robust Process for Large-Scale Synthesis of 4-Methylenepiperidine Hydrochloride , Letters in Organic Chemistry 2019; 16 (10) . https://dx.doi.org/10.2174/1876402910666181030094143