Convenient new synthesis of umeclidinium bromide |
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| Authors: | Jianhui Gu Jie Zhang Xuan Wang |
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| Affiliation: | 1. China State Institute of Pharmaceutical Industry, Shanghai, China;2. YangZhou Aurisco Pharmaceutical Co., Ltd, Yangzhou, China;3. Internship at China State Institute of Pharmaceutical Industry, Shanghai, China |
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| Abstract: | Umeclidinium bromide, a drug used for chronic obstructive pulmonary disease, is synthesized through a new intermediate of phenyl(quinuclidin-4-yl)methanone. This novel method with simple operation flow and cheap reagents, makes it suitable for scale up. The overall four-step process provides umeclidinium bromide in 29% yield and the purity up to 99.83%. The X-ray crystal structure of the drug molecule was first reported. |
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| Keywords: | Convenient synthesis crystal structure phenyl(quinuclidin-4-yl)methanone umeclidinium bromide |
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