Microreactor in the synthesis of active ingredients pharmaceuticals: synthesis of pro-2-yny 2-(lH-indol-3-yl)-2-oxoacetate

• Grant number: 15/21056-0
• Support Opportunities: Scholarships in Brazil - Scientific Initiation
• Start date: November 01, 2015
• End date: March 26, 2017
• Field of knowledge: Engineering - Chemical Engineering - Chemical Technology
• Principal Investigator: Mauri Sergio Alves Palma
• Grantee: Guilherme Leão de Azevedo Soter
• Host Institution: Faculdade de Ciências Farmacêuticas (FCF). Universidade de São Paulo (USP). São Paulo , SP, Brazil

Abstract

Microreactors offer excellent heat and mass transfer, high surface/volume ratio with laminar flow and without axial dispersion. Microreactor have been used in the continuous-flow synthesis of pharmaceuticals, creating chemical libraries of compounds with pharmacological potential, continuous synthesis in multiple steps, particularly for rapid reactions that involve much heat, intensive chemical processes and reactions with very dangerous, toxic or explosive chemicals. Some advantages of drug synthesis in microreactors are the drastic reduction of reaction times, due to the elimination of inefficient mixing effects, increased yield and selectivity of the reactions and reduction of waste generation. The Chemical-Pharmaceutical Industry is the largest beneficiary of this new technology, because the microreactors can generate a number of compounds with pharmacological potential, several orders of magnitude greater than in traditional batch process, can lessen in years the time for commercial production of a new drug and can be extremely small and compact industrial units. This work aims at using a microreactor to produce the indole derivative with propargyl alcohol that have biological activity and can become a drug. So far it was not found in the literature no information about that synthesis on micro reactor. Its production in continuous process has many advantages including higher yields, safety, productivity, selectivity and lower production cost. It will be determined the reaction kinetics and the best operating conditions of the synthesis in terms of temperature and residence time in the micro reactor. This project will be developed in the basis of the Regular Individual Financial Support approved by Fapesp process n. 2014/07757-2 supervised by Prof. Sergio Mauri Alves and valid from 9/1/2014 through 8/30/2016.