A Simple and Robust Process for Large-Scale Synthesis of 4-Methylenepiperidine Hydrochloride
Keyword(s):
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.
2003 ◽
Vol 377
(1-2)
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pp. 55-59
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Keyword(s):
2004 ◽
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pp. 3058-3062
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pp. 649-654
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pp. 1418-1422
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pp. 2603-2607
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pp. 879-889
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