A facile method for the synthesis of 2-(3-hydroxy-1-adamantyl)-2-oxoacetic acid and it's optimization

被引：0

作者：

Wang, Hui-fei ^{[1
]}

Gan, Run ^{[2
]}

Zhou, Jing ^{[1
]}

Liao, Qi ^{[1
]}

Wang, Tian-bao ^{[1
]}

Zhong, Cai-ling ^{[1
]}

Xiang, Yuan-yuan ^{[1
]}

Lin, Hong-bo ^{[1
]}

Hu, Xiang-nan ^{[1
]}

机构：

[1] Chongqing Med Univ, Dept Pharm, Chongqing, Peoples R China

[2] Bishan Area Maternal & Child Hlth Care Hosp, Chongqing, Peoples R China

来源：

PAKISTAN JOURNAL OF PHARMACEUTICAL SCIENCES | 2018年 / 31卷 / 04期

关键词：

Diabetes; key intermediate; saxagliptin; optimization; one-pot method; PEPTIDASE-IV INHIBITOR; SAXAGLIPTIN; INTERMEDIATE;

D O I：

暂无

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

2-(3-hydroxy-1-adamantyl)-2-oxoacetic acid (IV), a key intermediate of saxagliptin for type 2 diabetes mellitus (T2DM), was prepared from 1-adamantanecarboxylic acid(I) via oxidation by potassium permanganate(KMnO4) to afford 3-hydroxy-1-adamantanecarboxylic acid (II), which was treated with a one-pot method to give 1-acetyl-3-hydroxyadamantane (III) followed by oxidation. Some key steps were optimized and the overall yield was about 51%.

引用

页码：1393 / 1397

页数：5

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