非奈利酮的新合成路线
New Synthetic Route of Finerenone
于均超 1孟玲 1王婧 1吴庆昆 2钱思甜1
作者信息
- 1. 连云港职业技术学院,江苏省药物递送载体材料工程技术研究开发中心,江苏连云港 222000
- 2. 江苏海洋大学药学院,江苏省海洋药物活性分子筛选重点实验室,江苏连云港 222005
- 折叠
摘要
以二乙烯酮和对甲氧基苄胺为起始原料,经胺解、缩合、Hantzsch关环、乙基化和手性拆分等步骤,得到非奈利酮(1),并优化了反应条件.该工艺总收率11.4％,纯度99.7％.该路线的新颖之处是首次引入对甲氧基苄基保护基,适合工业化生产.
Abstract
Finerenone(1)was synthesized from diketene and 4-methoxybenzylamine as the starting materials,through the aminolysis,condensation,Hantzsch cyclization,ethylation,and chiral resolution steps.After optimizing the reaction conditions,the overall yield of this process was 11.4％with the purity of 99.7％.The usage of 4-methoxybenzyl group as the protection group was reported at the first time in this route,which was suitable for industrial production.
关键词
非奈利酮/合成/糖尿病肾病/选择性盐皮质激素受体拮抗药Key words
finerenone/synthesis/diabetic nephropathy/selective mineralocorticoid receptor antagonist引用本文复制引用
出版年
2024
NETL
NSTL
万方数据