A Simple and Robust Process for Large-Scale Synthesis of 4-Methylenepiperidine Hydrochloride-Reference-Cited by-同舟云学术

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

Published:2019-08-23 Issue:10 Volume:16 Page:802-806
ISSN:1570-1786
Container-title:Letters in Organic Chemistry
language:en
Short-container-title:LOC

Author:

Chen Ao¹,Li Ziqian²,Li Minghai¹,Liu Keke¹,Li Weimin³,Tan Chen⁴

Affiliation:

1. Shanghai Pharma Group Changzhou Kony Pharmaceutical Co. Ltd., Changzhou, 213105, China

2. Undergraduate Department, University of Chinese Academy of Sciences, Beijing, 100049, China

3. School of Petrochemical Engineering, Changzhou University, Changzhou 213164, China

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

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.

Funder

Advanced Catalysis and Green Manufacturing Collaborative Innovation Center

Publisher

Bentham Science Publishers Ltd.

Subject

Organic Chemistry,Biochemistry

Reference14 articles.

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