Synthesis in flow of lobeglitazone

• Grant number: 18/11970-4
• Support Opportunities: Scholarships in Brazil - Scientific Initiation
• Start date: August 01, 2018
• End date: December 31, 2019
• Field of knowledge: Engineering - Chemical Engineering - Chemical Technology
• Principal Investigator: Mauri Sergio Alves Palma
• Grantee: Leandro Leite Reche
• Host Institution: Faculdade de Ciências Farmacêuticas (FCF). Universidade de São Paulo (USP). São Paulo , SP, Brazil

Abstract

Type 2 diabetes mellitus affects more than 400 million people around the world with a prospective increase in the number of patients of more than 640 million in 2040. The disease is characterized mainly by excess glucose in the blood due to irregular and insufficient secretion of insulin, and Lobeglitazone, a compound of the class of glitazones that functions as an insulin sensitizer in humans, stands out among the drugs used in its treatment. Its synthesis will be carried out in batch or continuous flow microreactor. When compared to batch reactors, the Microreactor Technology (TMR) has as main advantages the substantial reduction of residues and impacts generated by the process and the significant increase of mass and heat transfer rates, which results in the ease of control of process, allowing higher yields and selectivity of chemical reactions. This research project aims to study the three final steps of the process of obtaining Lobeglitazone, first in a batch reactor and then in a continuous flow capillary microreactor. It also seeks to define the best operating conditions in terms of temperature, solvent, catalyst, catalyst concentration and total concentration of the reaction medium in the two reactor, and additionally the optimal reaction time in the batch process, which corresponds to the mean residence time in the microreactor. The values of these variables will be determined in order to maximize the conversion of the limiting reagent, yield and selectivity of the product.