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The Research of the Preparation Process of Asthma Drug, Pranlukast

Author: ShiGang
Tutor: WuFanHong；ZhaoMin
School: East China University of Science and Technology
Course: Organic Chemistry
Keywords: Pranlukast Pot reaction Synthesis Cyanuric chloride
CLC: TQ463.53
Type: Master's thesis
Year: 2011
Downloads: 179
Quote: 0
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Abstract


This paper is a to confrontation the asthma drug Pranlukast synthetic process improved research and development . In this thesis, the present group of students synthetic preparation of two important intermediate 4 - phenyl - 1 - bromobutane and 3 - amino-2 - hydroxyacetophenone hydrochloride as a starting material . After etherification, hydrolysis , amidation , ketoester condensation , cyclization, aminolysis , amide dehydration into cyanide, and then with sodium azide to give the object product pranlukast . Synthesis method reported Pranlukast compared with the reported preparation process of this thesis, the research and development process has the following characteristics : cheap and easy to get raw materials ; reduce the reaction step , easy to operate ; multi-step reaction can get a higher yield , reduce byproducts , to avoid the emission of harmful substances ; mild operating conditions of each reaction , the optimization of the production process , reduce costs ; total yield of 42.3% . Wherein the two-step reaction of the keto ester condensation cyclization combined pot method is complete , reducing the amount of the solvent to shorten the reaction time , the reaction product can be achieved a yield of 93% of the HPLC detection purity more than 99% , and achieved good results . In the preparation of 8 - [4 - ( 4 - butyloxy phenyl ) benzoyl ] amine -4 - oxy -4H-1- benzopyran-2 - carbonitrile , using cyanuric chloride as a dehydrating agent , cheaper and environmentally friendly than the phosphorus compounds , the products were determined by HPLC purity of more than 98% , and is suitable for industrial production .

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CLC: > Industrial Technology > Chemical Industry > Pharmaceutical chemical industry > Production of organic compounds in drug > Heterocyclic compounds drugs > Five section heterocyclic
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