Levodropropizine, an antitussive drug, was prepared in high enantiomeric excess in three steps, starting from dichloroacetone (2).Monosubstitution of 2 with sodium benzoate and subsequent baker’s yeast reduction stereoselectively afforded the correspondingchlorohydrin in 73% ee, which was converted to levodropropizine and enantiomerically enriched up to 95% ee by fractionalcrystallisation
Chemo-enzymatic synthesis of levodropropizine / Caselli, Emilia; Tosi, Giovanni; Forni, Arrigo; Bucciarelli, Maria; Prati, Fabio. - In: IL FARMACO. - ISSN 0014-827X. - STAMPA. - 58:10(2003), pp. 1029-1032. [10.1016/S0014-827X(03)00189-7]
Chemo-enzymatic synthesis of levodropropizine
CASELLI, Emilia;TOSI, Giovanni;FORNI, Arrigo;BUCCIARELLI, Maria;PRATI, Fabio
2003-01-01
Abstract
Levodropropizine, an antitussive drug, was prepared in high enantiomeric excess in three steps, starting from dichloroacetone (2).Monosubstitution of 2 with sodium benzoate and subsequent baker’s yeast reduction stereoselectively afforded the correspondingchlorohydrin in 73% ee, which was converted to levodropropizine and enantiomerically enriched up to 95% ee by fractionalcrystallisation
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