CN Patent

CN110776512A — 一种核苷类似物的制备方法

Assigned to CHENGDU AF BIOCHEM Co Ltd · Expires 2020-02-11 · 6y expired

What this patent protects

本发明属于化学品合成技术领域,具体涉及(2R,3R,4S,5R)‑2‑(4‑氨基吡咯并[1,2‑f][1,2,4]三嗪‑7‑基)‑3,4‑二羟基‑5‑(羟基甲基)四氢呋喃‑2‑甲腈新的制备方法,具体步骤:1)以2,3,5‑三苄氧基‑D‑核糖酸‑1,4‑内酯和4‑氨基‑7‑溴吡咯并[2,1‑f][1,2,4]三嗪为原料合成中间体I;2)通过中间体I制得中间体II;3)将制得的中间体II直接溶于二氯甲烷,降温‑15℃以下,滴加三氯化硼,反应结束后,使用甲醇淬灭,减压浓缩后,加入甲醇与水的混合溶液,调节pH至7,搅拌过夜,析出的固体化合物即得。本发明的制备方法…

USPTO Abstract

本发明属于化学品合成技术领域,具体涉及(2R,3R,4S,5R)‑2‑(4‑氨基吡咯并[1,2‑f][1,2,4]三嗪‑7‑基)‑3,4‑二羟基‑5‑(羟基甲基)四氢呋喃‑2‑甲腈新的制备方法,具体步骤:1)以2,3,5‑三苄氧基‑D‑核糖酸‑1,4‑内酯和4‑氨基‑7‑溴吡咯并[2,1‑f][1,2,4]三嗪为原料合成中间体I;2)通过中间体I制得中间体II;3)将制得的中间体II直接溶于二氯甲烷,降温‑15℃以下,滴加三氯化硼,反应结束后,使用甲醇淬灭,减压浓缩后,加入甲醇与水的混合溶液,调节pH至7,搅拌过夜,析出的固体化合物即得。本发明的制备方法收效高,副产物较少,能够高效,大规模放量生产(2R,3R,4S,5R)‑2‑(4‑氨基吡咯并[1,2‑f][1,2,4]三嗪‑7‑基)‑3,4‑二羟基‑5‑(羟基甲基)四氢呋喃‑2‑甲腈。

Drugs covered by this patent

Patent Metadata

Patent number
CN110776512A
Jurisdiction
CN
Classification
Expires
2020-02-11
Drug substance claim
No
Drug product claim
No
Assignee
CHENGDU AF BIOCHEM Co Ltd
Source
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