Beilstein J. Org. Chem.2015,11, 2641–2645, doi:10.3762/bjoc.11.283
., Shanghai 201203, China 10.3762/bjoc.11.283 Abstract A novel and practical asymmetric synthesis of dapoxetinehydrochloride by using the chiral auxiliary (S)-tert-butanesulfinamide was explored. The synthesis was concise, mild, and easy to perform. The overall yield and stereoselectivity were excellent
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Keywords: asymmetric synthesis; dapoxetinehydrochloride; stereoselectivity; (S)-tert-butanesulfinamide; Introduction
Premature ejaculation (PE) is the most frequent form of ejaculatory dysfunction with a distribution of 39% of the general male population [1][2]. Dapoxetinehydrochloride (1, (S)-(+)-N,N
synthesis of this interesting drug has attracted great attention, especially asymmetric synthesis approaches. However, only a few methods have been reported for the synthesis of enantiopure dapoxetinehydrochloride. The earlier methods included chiral/enzymatic resolution [5], whereas the newer approaches