- Synthesis method of (S)-3-(4-chlorophenyl)-piperidine
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The invention relates to a synthetic method of (S)-3-(4-chlorophenyl)-piperidine. The invention mainly aims to solve the technical problems of harsh reaction conditions, expensive catalysts, high cost, unsuitability for large-scale production and the like when optically pure (S)-3-(4-chlorophenyl)-piperidine is prepared by hydrogenating a pyridine ring and then utilizing chiral SFC. The synthesis method comprises the following four steps: (1) alpha-site alkylation of 4-chlorobenzyl cyanide; (2) reduction of 5-chloro-2-(4-chlorophenyl)valeronitrile; (3) cyclization of the 5-chloro-2-(4-chlorphenyl)amyl-1-amine to obtain (RS)-3-(4-chlorophenyl)-piperidine; and (4) chemical resolution of the (RS)-3-(4-chlorophenyl)-piperidine to obtain a final product. A target product with an optical purity reaching 98% or above is obtained through four-step reaction. The method is high in yield, low in cost, simple and convenient to operate and purify, good in economic benefits and more suitable for industrial production.
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Paragraph 0006; 0009; 0011; 0015-0016
(2021/05/12)
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- QUATERNARY LACTAM COMPOUND AND PHARMACEUTICAL USE THEREOF
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A quaternary lactam compound of formula (I). The compound is used in the manufacture of a medicament for the treatment and/or prevention of thrombotic or thromboembolic disorders.
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