Abstract
An optimized convergent synthetic route for the preparation of retinoid X receptor (RXR) antagonist (1) in an overall yield of 35% is described. The formation of the benzodiazepine was achieved in 85% yield using POCl3 in toluene. The drug substance 14 was obtained by treatment of aryl bromide with vinyl butyl ether in the presence of palladium acetate, DPPP, and cesium carbonate This one-pot operation incorporating three chemical transformations (i.e., Heck reaction, hydrolysis of vinyl ether, and hydrolysis of ester) was achieved in 85% yield.
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