Synthesis of rosiglitazone intermediates in batch process and capillary microreactor

• Grant number: 17/24441-7
• Support Opportunities: Scholarships in Brazil - Scientific Initiation
• Effective date (Start): February 01, 2018
• Effective date (End): December 31, 2018
• Field of knowledge: Engineering - Chemical Engineering - Chemical Technology
• Principal Investigator: Mauri Sergio Alves Palma
• Grantee: Paulo Victor Cuesta Calvo
• Host Institution: Faculdade de Ciências Farmacêuticas (FCF). Universidade de São Paulo (USP). São Paulo , SP, Brazil

Abstract

The use of microreactors in the chemical-pharmaceutical industries provides the reduction of the impact generated by the processes with substantial waste reduction. In addition, they provide an expressive increase in mass and heat transfer rates, which results in an easily controllable process allowing greater throughput and selectivity compared to batch reactors. Considering these characteristics, it is imperative that the Microreactor Tecnology (MRT) is more widespread in the chemical-pharmaceutical industry, since it is necessary to increase the scale of production to attend the market demand in a faster and more efficient way, and thus recover the applied during the research. Diabetes mellitus is a chronic metabolic disorder characterized by excess blood glucose due to lack of insulin secretion, insufficient insulin causes deficiencies in the metabolism of carbohydrates, lipids and proteins. Rosiglitazone is one of the antiglucemic agents from the class of glitazones used in the fight against diabetes mellitus type 2, and acts as an insulin sensitizer in humans. The present work aims the transposition of one intermediate reaction of the four necessary for the synthesis of Rosiglitazone from the usual process in the chemical-pharmaceutical industry (batch) for the continuous flow in capillary microreactor. In addition, it aims to define the best operating conditions in terms of temperature, solvent, catalyst, catalyst concentration and total reactional medium concentration for both processes and also the reaction time in the batch process, which corresponds to the average residence time in the microreactor, in order to maximize the conversion of the limiting reagent, product yield and selectivity. This project will be developed within the scope of individual aid to research funded by Fapesp no. 2017/128309 entitled "Synthesis of Pioglitazone, Rosiglitazone and Loboglitazone in continuous flow in capillary microreactors" in effect from 10/01/2017 to 09/30/2019. (AU)