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Title: A stereoselective, catalytic strategy for the in-flow synthesis of advanced precursors of rasagiline and tamsulosin
Authors: Burke, Anthony J
Benaglia, Maurizio
Brenna, Davide
Pirola, Margherita
Raimondi, Laura
Editors: Waldmann, Herbert
Keywords: Flow Chemistry
Active Pharmaceutical ingredient
Issue Date: 1-Dec-2017
Publisher: Elsevier
Abstract: The diastereoselective, trichlorosilane-mediate reduction of imines, bearing different and removable chiral auxiliaries, in combination either with achiral bases or catalytic amounts of chiral Lewis bases, was investigated to afford immediate precursors of chiral APIs (Active Pharmaceutical Ingredients). The carbon-nitrogen double bond reduction was successfully performed in batch and in flow mode, in high yields and almost complete stereocontrol. By this metal-free approach, the formal synthesis of rasagiline and tamsulosin was successfully accomplished in micro(meso) flow reactors, under continuous flow conditions. The results of these explorative studies represent a new, important step towards the development of automated processes for the preparation of enantiopure biologically active compounds
URI: 10.1016/j.bmc.2017.01.023
ISSN: 0968-0896
Type: article
Appears in Collections:CQE - Publicações - Artigos em Revistas Internacionais Com Arbitragem Científica

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