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

作者：Chen, Ao; Li, Zigian; Li, Minghai; Liu, Keke; Li, Weimin; Tan, Chen^*

来源：Letters in Organic Chemistry, 2019, 16(10): 802-806.

DOI：10.2174/1876402910666181030094143

• 4-methylenepiperidine hydrochloride
• efinaconazole
• drug
• intermediate
• synthetic process
• large-scale

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.

• 出版日期2019
• 单位中国科学技术大学; 常州大学; 中国科学院大学