Abstract
Celgene’s Otezla® 1 (apremilast) is the first and only PDE4 inhibitor approved by the US FDA for the treatment of plaque psoriasis and psoriatic arthritis. The active pharmaceutical ingredient 1 has been historically prepared via resolution to obtain the enantioenriched aminosulfone intermediate. Herein we have investigated the use of catalytic asymmetric hydrogenation for the enantioselective synthesis of the key aminosulfone intermediate in order to identify a higher yielding and greener synthesis route. Asymmetric reduction of enamine 7 and ketone 11 both proceeded with high selectivity, generating their respective products with >95% ee.
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