Development of flow chemistry synthetic platform to obtain molecules of pharmaceutical interest

• Grant number: 15/11801-0
• Support Opportunities: Research Grants - Innovative Research in Small Business - PIPE
• Start date: February 01, 2016
• End date: January 31, 2018
• Field of knowledge: Physical Sciences and Mathematics - Chemistry - Organic Chemistry
• Agreement: FINEP - PIPE/PAPPE Grant
• Principal Investigator: Leandro de Carvalho Alves
• Grantee: Leandro de Carvalho Alves
• Company: Accert Indústria, Comércio, Importação e Exportação em Química e Biotecnologia Ltda
• City: São Carlos
• Associated researchers: Kleber Thiago de Oliveira ; Marco Antonio Barbosa Ferreira
• Associated scholarship(s): 16/01497-4 - Development of flow chemistry synthetic platform to obtain molecules of pharmaceutical interest, BP.PIPE

Abstract

This research project aims to develop continuous flow chemistry platforms to obtain the molecules Pravastatin, their sodium and ammonium salts, and Eslicarbazepine, Eslicarbazepine acetate and Carbamazepine epoxy, degradation products of assets Carbamazepine and simvastatin, respectively. These molecules are strategic for the pharmaceutical industry in order to meet the current legislation such as RDC Resolution 58/2013 (ANVISA), which establishes parameters degradation products studies in pharmaceutical formulations. In this sense, we believe that the development of flow chemistry platforms may provide a unique and high value-added technology. These platforms allow a high efficient conversion of raw materials into products. They also provide high-levels of chemical syntheses automation and an improvement in the hydrogenation processes safety. Reduction in processes spending energy and management of minimized generated waste are on the spotlights as well. Furthermore, the development of this technology will certainly contribute to Brazilian fine chemicals trade balance, which was negative of nearly $ 9.0 billion in 2013. We intend to use as a primary source of raw materials both drugs and medicines recycled throughout our Pharmaceuticals Recycling Project (FAPESP 2012 / 51338-9) currently in the final steps at Accert Chemistry and Biotechnology. Accert already sells (exports) products developed in partnership with FAPESP (process 2010 / 51662-5) for a major Swiss customer, a global leader in the marketing of high-purity analytical standards. So we have a real direction of the current market demand for this type of substance. In addition, we have the formal support of one of our customers in the pharmaceutical market, a national industry leader, in order to support the project and scale up processes development after Phase 2 Project. (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)

DE SOUZA, ALINE A. N.; BARTOLOMEU, ALOISIO DE A.; BROCKSOM, TIMOTHY J.; NOEL, TIMOTHY; DE OLIVEIRA, KLEBER T.. Direct Synthesis of ?-Sulfenylated Ketones under Electrochemical Conditions br. Journal of Organic Chemistry, v. 87, n. 9, p. 10-pg., 2022-05-06. (15/11801-0, 19/27176-8, 13/07276-1, 20/06874-6)

MARTINS, GUILHERME M.; MAGALHAES, MARIA F. A.; BROCKSOM, TIMOTHY J.; BAGNATO, VANDERLEI S.; DE OLIVEIRA, KLEBER T.. Scaled up and telescoped synthesis of propofol under continuous-flow conditions. JOURNAL OF FLOW CHEMISTRY, v. 12, n. 3, p. 9-pg., 2022-07-19. (13/07276-1, 15/11801-0, 19/27176-8, 20/06874-6, 21/01259-4)

CARMONA-VARGAS, CHRISTIAN C.; ALVES, LEANDRO DE C.; BROCKSOM, TIMOTHY J.; DE OLIVEIRA, KLEBER T.. Combining batch and continuous flow setups in the end-to-end synthesis of naturally occurring curcuminoids. REACTION CHEMISTRY & ENGINEERING, v. 2, n. 3, p. 366-374, JUN 2017. (11/13993-2, 13/07276-1, 15/21110-4, 15/11801-0)