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发明公开
CN107574194A 生物催化制备(R)-1-N-苯甲氧羰基-3-羟基哌啶的方法 无效 - 撤回 转让

生物催化制备(R)-1-N-苯甲氧羰基-3-羟基哌啶的方法
摘要：
本发明涉及生物催化制备(R)-1-N-苯甲氧羰基-3-羟基哌啶（以下简称(R)-N-Cbz-3-羟基哌啶）的方法。主要解决现有制备方法均以叔丁氧羰基作为保护基团在弱酸性条件下稳定性较差的技术问题。本发明的技术方案：一种(R)-N-Cbz-3-羟基哌啶的制备方法，在以异丙醇或/和葡萄糖作为氢源，醇脱氢酶作为辅酶的条件下，通过酶催化转化1-N-苯甲氧羰基-3-哌啶酮直接制备式II的(R)-N-Cbz-3-羟基哌啶；反应式如下：。
摘要（英）：

The invention relates to a method for preparing (R)-1-N-carbobenzoxy-3-hydroxypiperidine (hereinafter referred to as (R)-N-Cbz-3-hydroxypiperidine) by biological catalysis, mainly aiming at solving the technical problems of an existing preparation method that tert-butoxycarbonyl is used as a protection group and the stability under a weak acidic condition is relatively poor. According to the technical scheme provided by the invention, the preparation method of the (R)-N-Cbz-3-hydroxypiperidine) comprises the step of directly preparing the (R)-N-Cbz-3-hydroxypiperidine shown as a formula II through carrying out enzyme catalysis conversion on 1-N-carbobenzoxy-3-piperidone under the condition that isopropyl alcohol or/glucose is used as a hydrogen source and alcohol dehydrogenase is used as acoenzyme, wherein a reaction formula is as follows: the formula is shown in the description.

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