Convenient new synthesis of umeclidinium bromide

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

KEYWORDS:

• Convenient synthesis
• crystal structure
• phenyl(quinuclidin-4-yl)methanone
• umeclidinium bromide