Integrated consecutive high-T, high-p Novel Process Windows for flow chemistry synthesis of Dihydropyrines (DHP)

• Grant number: 11/20268-2
• Support Opportunities: Scholarships abroad - Research
• Start date: May 01, 2012
• End date: November 30, 2012
• Field of knowledge: Physical Sciences and Mathematics - Chemistry - Organic Chemistry
• Principal Investigator: Patrícia Tambarussi Baraldi
• Grantee: Patrícia Tambarussi Baraldi
• Host Investigator: Volker Hessel
• Host Institution: Instituto Vita Nova (IVN). Hortolândia , SP, Brazil
• Institution abroad: Eindhoven University of Technology (TU/e), Netherlands

Abstract

The present proposal aims at significant and strategic advantages by trying to increase the ability of pharmaceutical ingredients production on a national scale. To develop this new technology or new paradigm Novel Process Windows - NPW, aiming at a future decrease of import of these high values active pharmaceutical ingredients. The development of new innovative drugs involves high budgets and high risk of failure, due to the low probability of a lead of drug to begin at the market. However the necessity to obtain material and information for commercialization, including scale-up, show the authenticity of the chemical process, even before this drug obtains endorsement as a drug (Laird, 2007). In this way it is interesting to think about obtaining more compounds faster and efficient for screening pharmacological activity in early drug development, decreasing time to get Clinic Phases 1 or 2, and lowering challenges in scale-up in usual batch process. The 1,4-dihidropyridines (DHP) are bioactive compounds, clinically used against aging and hyperstion (Gordeev, 1998). So, in this way this project aims to obtain DHP´s as Darodipina (9) and Elgodipina (11) employing micro-reactors and a flow continuous process of integrated steps, to obtain a safer, effective and economic chemical process in order to prepare these compound classes. Also, aiming at patents and scientific papers. (AU)

Scientific publications

(References retrieved automatically from Web of Science and SciELO through information on FAPESP grants and their corresponding numbers as mentioned in the publications by the authors)

BARALDI, PATRICIA TAMBARUSSI; NOEL, TIMOTHY; WANG, QI; HESSEL, VOLKER. The accelerated preparation of 1,4-dihydropyridines using microflow reactors. Tetrahedron Letters, v. 55, n. 13, p. 2090-2092, MAR 26 2014. (11/20268-2)

BARALDI, PATRICIA T.; HESSEL, VOLKER. Micro reactor and flow chemistry for industrial applications in drug discovery and development. GREEN PROCESSING AND SYNTHESIS, v. 1, n. 2, p. 149-167, APR 2012. (11/20268-2)