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非奈利酮的新合成路线

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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.
New Synthetic Route of Finerenone
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.

finerenonesynthesisdiabetic nephropathyselective mineralocorticoid receptor antagonist

于均超、孟玲、王婧、吴庆昆、钱思甜

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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

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

非奈利酮 合成 糖尿病肾病 选择性盐皮质激素受体拮抗药

2024

中国医药工业杂志
上海医药工业研究院,中国化学制药工业协会

中国医药工业杂志

CSTPCD
影响因子:0.487
ISSN:1001-8255
年,卷(期):2024.55(12)