Synthesis And Process Optimization Of The Chiral Intermediate Of Montelukast

Montelukast is a leukotriene receptor antagonist (LTRAs).It was developed by Merck of USA which used mainly for the treatment of asthma and allergies.It is one of the LTRAs that received wide international attention now.This paper mainly introduces the process optimization of the montelukast chiral alcohol intermediate.The chemical name of the intermediate is 2-(3-(3-((E)2-(7-chloroquinolin-2-yl)ethenyl)phenyl)-3(S)-hydroxypropyl)benzoic acid methyl ester. As the report in the literatures as the basis,We conducted a further optimization of the process of the chiral alcohol intermediate. The main idea of the research is about to optimize the temperature and time of the reaction, simplify the operation and substitute or quantify the raw materials in order to get a better route of industrialization. Finally,we open up the process route while fully optimize the process.At the same time,we also confirm the stability of the reaction process by some pilot plant tests.The main purpose of this thesis is to set up a safe,environmental and economic industrialized production line. We focus on the asymmetric reduction process in the total research.The preparation and standardization of the reductor and simplification of the reduction reaction is more important in this discuss.