利索-全球专利检索

  1. 登录
  2. 注册
发明公开
CN109971802A 一种酶法拆分制备(S)-1,2,3,4-四氢异喹啉-1-甲酸及其衍生物的方法 有权

一种酶法拆分制备(S)-1,2,3,4-四氢异喹啉-1-甲酸及其衍生物的方法
摘要：
本发明公开了一种酶法拆分制备(S)‑1,2,3,4‑四氢异喹啉‑1‑甲酸及其衍生物的新方法，所述方法为：以外消旋1,2,3,4‑四氢异喹啉‑1‑甲酸(1)或外消旋6,7‑二甲氧基‑1,2,3,4‑四氢异喹啉‑1‑甲酸(2)为底物，利用离体的D‑氨基酸氧化酶或胞内表达D‑氨基酸氧化酶的细胞作为催化剂，选择性催化(R)‑1,2,3,4‑四氢异喹啉‑1‑甲酸或(R)‑6,7‑二甲氧基‑1,2,3,4‑四氢异喹啉‑1‑甲酸的氧化脱氢反应，(S)‑1,2,3,4‑四氢异喹啉‑1‑甲酸或(S)‑6,7‑二甲氧基‑1,2,3,4‑四氢异喹啉‑1‑甲酸未被催化，保留在反应体系中，由此制备获得(S)‑1,2,3,4‑四氢异喹啉‑1‑甲酸或(S)‑6,7‑二甲氧基‑1,2,3,4‑四氢异喹啉‑1‑甲酸。本发明方法转化率>49％，ee值>99％，具有反应条件温和、立体选择性强、反应效率高、工艺相对简单等特点。
摘要（英）：

The present invention discloses a novel method for preparing (S)-1,2,3,4-tetrahydroisoquinoline-1-formic acid and derivatives thereof by enzymatic resolution. The method is as follows: racemic 1,2,3,4-tetrahydroisoquinoline-1-formic acid (1) or racemic 6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline-1-formic acid (2) is used as a substrate, isolated D-amino acid oxidase or cells expressing the D-amino acid oxidase intracellularly are used as a catalyst to conduct selective catalysis of oxidative dehydrogenation of (R)-1,2,3,4-tetrahydroisoquinoline-1-formic acid or (R)-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline-1-formic acid, (S)-1,2,3,4-tetrahydroisoquinoline-1-formic acid or (S)-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline-1-formic acid are not catalyzed and remain in the reaction system,and thus the (S)-1,2,3,4-tetrahydroisoquinoline-1-formic acid or (S)-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline-1-formic acid are obtained. The method has a conversion rate larger than 49% and an ee value larger than 99%, and has characteristics of mild reaction conditions, strong stereoselectivity, high reaction efficiency, relatively simple processes, etc.

公开/授权文献
0/0