Applications of the Aza-Michael Reaction in Flow Chemistry for the Synthesis of API

Author

Alkayal, Housam

Abstract

Different specific reaction conditions of the aza-Michael reaction are explored, which can be used in combination with flow chemistry to improve industrial API production. This project involves the use of different Michael acceptors and aza-type donors, to expand the applicability of the method in collaboration with an industrial company. For this, the work includes the use of 4-vinylpyridine and different amines, both in batch and in flux, to make a direct comparison between them. Furthermore, the results are compared with those obtained with 2-vinylpyridine, also in batches and in flow. It is observed that the behavior of the mixture of 4-vinylididine with the aqueous solution of an amine salt provides a single phase, unlike 2-vinylpyridine, which gives two, this fact may be due to the formation of micelles. Previous work with 2-vinylpyridine has shown that increasing the temperature improves its performance and selectivity. However, for 4-vinylpyridine, the increase in temperature causes the yields to decrease. The best conversion, yield and selectivity results are obtained by increasing the residence time in the flow reactor.

 

Director

Sempere Cebriàn, Julià

Degree

IQS SE - Master’s Degree in Pharmaceutical Chemistry

Date

2021-09-21