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



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.
