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

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

Journal Name: Letters in Organic Chemistry

Volume 16 , Issue 10 , 2019

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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.

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

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Article Details

Year: 2019
Page: [802 - 806]
Pages: 5
DOI: 10.2174/1876402910666181030094143
Price: $95

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