Please use this identifier to cite or link to this item: http://localhost:80/xmlui/handle/123456789/16191
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
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