A new route to Roflumilast via copper-catalyzed hydroxylation
A new route to Roflumilast, a selective phosphodiesterase type 4 (PDE 4) inhibitor, is described. The synthetic procedure starts from 4-hydroxy-3-iodobenzoic acid to access the key intermediate 3- (cyclopropylmethoxy)-4-(difluoromethoxy)benzoic acid via copper-catalyzed hydroxylation and utilizes amide coupling to accomplish the synthesis of Roflumilast in 80% overall yield. Georg Thieme Verlag KG Stuttgart · New York.
Ni, Feng,Li, Jianqi
p. 3598 - 3602
(2013/02/22)
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