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- Title
A facile method for the synthesis of 2-(3-hydroxy-1-adamantyl)-2-oxoacetic acid and it's optimization.
- Authors
Hui-fei Wang; Run Gan; Jing Zhou; Qi Liao; Tian-bao Wang; Cai-ling Zhong; Yuan-yuan Xiang; Hong-bo Lin; Xiang-nan Hu
- Abstract
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%.
- Subjects
TYPE 2 diabetes treatment; POTASSIUM permanganate; PEOPLE with diabetes; OXALYL chloride; OXIDATION
- Publication
Pakistan Journal of Pharmaceutical Sciences, 2018, Vol 31, Issue 4, p1393
- ISSN
1011-601X
- Publication type
Article