Synthetic method of improved 1-benzyl-3-piperidinol intermediate

The invention discloses a synthetic method of an improved 1-benzyl-3-piperidinol intermediate. The synthetic method comprises the steps that 4-bromobutyraldehyde is used as a raw material, under the action of an R-apricot kernel oxynitrilase without being fixed with a carrier, and a cyan group trans...

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Bibliographische Detailangaben
Hauptverfasser: YANG SHUPING, WANG XIHONG, TENG SHITAO, XUE CHUNQI, ZHENG HAIXUAN
Format: Patent
Sprache:chi ; eng
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Zusammenfassung:The invention discloses a synthetic method of an improved 1-benzyl-3-piperidinol intermediate. The synthetic method comprises the steps that 4-bromobutyraldehyde is used as a raw material, under the action of an R-apricot kernel oxynitrilase without being fixed with a carrier, and a cyan group transfer reaction is performed with racemic hydrocyanic acids, so that the 1-benzyl-3-piperidinol intermediate is obtained. The synthetic method not only is high in three-dimensional selection, but also is high in yield. 本发明公开了一种改进的1-苄基-3-哌啶醇中间体合成方法,以4-溴丁醛为原料,在无载体固定的R-杏仁醇腈酶催化剂作用下与外消旋的氢氰酸供体进行氰基转移反应,得到1-苄基-3-哌啶醇中间体。该合成方法不仅立体选择较高,同时产率较高。