The accelerated preparation of 1,4-dihydropyridines using microflow reactors

Autor(es)

Baraldi, Patricia Tambarussi ^{[1, 2]} ; Noel, Timothy ^{[1, 3]} ; Wang, Qi ^[1] ; Hessel, Volker ^[1]

Afiliação do(s) autor(es)

^[1] Eindhoven Univ Technol, Dept Chem Engn & Chem Micro Flow Chem & Proc Tech, NL-5612 AZ Eindhoven - Netherlands

^[2] Inst Vita Nova, Hortolandia 13 - Brazil

^[3] Univ Ghent, Dept Organ Chem, B-9000 Ghent - Belgium

• Tipo de documento: Artigo Científico
• Fonte: Tetrahedron Letters; v. 55, n. 13, p. 2090-2092, MAR 26 2014.
• Citações Web of Science: 10

Resumo

The synthesis of 1,4-dihydropyridines was performed in a continuous-flow microreactor. Elevated temperatures accelerated the reaction rate significantly allowing the reaction to be finished in minutes (6-11 min). Different 1,4-dihydropyridines were prepared in good to excellent isolated yields (45-88% yield). The method was amenable to the preparation of daropidine, a calcium channel blocker which is currently in clinical phase 3 trials. (C) 2014 Elsevier Ltd. All rights reserved. (AU)

• Processo FAPESP: 11/20268-2 - Integração consecutiva de alta-T e alta-P em Novel Process Windows para a química em fluxo de Dihidropiridinas (DHP's)
• Beneficiário: Patrícia Tambarussi Baraldi
• Modalidade de apoio: Bolsas no Exterior - Pesquisa