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Synthetic Communications
An International Journal for Rapid Communication of Synthetic Organic Chemistry
Volume 48, 2018 - Issue 9
368
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Original Articles

Convenient new synthesis of umeclidinium bromide

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Pages 995-1000 | Received 05 Mar 2017, Published online: 07 May 2018
 

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.

GRAPHICAL ABSTRACT

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