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Title: | A facile method for the synthesis of 2-(3-hydroxy-1-adamantyl)-2oxoacetic acid and it’s optimization |
Authors: | Wang, Hui-fei Run Gan Jing Zhou Qi Liao Wang, Tian-bao Zhong, Cai-ling Xiang, Yuan-yuan Lin, Hong-bo Hu, Xiang-nan |
Keywords: | Diabetes key intermediate saxagliptin optimization one-pot method. |
Issue Date: | 20-Jul-2018 |
Publisher: | Karachi: Pakistan Botanical Society, University of Karachi |
Citation: | Wang, H. F., Gan, R., Zhou, J., Liao, Q., Wang, T. B., Zhong, C. L., ... & Hu, X. N. (2018). A facile method for the synthesis of 2-(3-hydroxy-1-adamantyl)-2-oxoacetic acid and it's optimization. Pakistan Journal of Pharmaceutical Sciences, 31(4). |
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% |
URI: | http://142.54.178.187:9060/xmlui/handle/123456789/16191 |
ISSN: | 1011-601X |
Appears in Collections: | Issue 04 |
Files in This Item:
File | Description | Size | Format | |
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Paper-26.htm | 132 B | HTML | View/Open |
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