专利号:WO-2013138200-A1 优先权日:2012-03-13 标 题 :Green chemistry synthesis of the malaria drug amodiaquine and analogs thereof 发明人:FORTUNAK JOSEPH MARIAN; KULKARNI AMOL ANANT; KING CHRISTOPHER 权利人:UNIV HOWARD 摘要:Methods are provided for a green chemistry one-pot synthesis of amodiaquine and amodiaquine analogs. The methods have a lower environmental impact, lower investment cost, reduced amounts of byproducts and impurities, and a shorter synthesis time, compared to current conventional synthesis methods. The methods reduce the total number of steps in the synthesis from four to five down to two, thereby simplifying production; and allow a reduced number of solvents and reagents to be used in production, thereby reducing the waste generated in the synthesis. The methods can reduce the waste to about 3-5 kilograms of waste generated per kilogram of product produced; and surprisingly improve the overall yield from 60-65% to greater than 90% as compared to the current conventional synthesis methods for amodiaquine and its analogs.
专利号:CN-114292232-A 优先权日:2022-01-26 标题:A kind of synthesis and purification method of 4,7-dichloroquinoline
参考标题: Green Chemistry Synthesis Of The Malaria Drug Amodiaquine And Analogs Thereof Synthèse De Chimie Verte Du Médicament Contre Le Paludisme, L'Amodiaquine Et Ses Analogues 摘要:Methods Are Provided For A Green Chemistry One-Pot Synthesis Of Amodiaquine And Amodiaquine Analogs. The Methods Have A Lower Environmental Impact, Lower Investment Cost, Reduced Amounts Of Byproducts And Impurities, And A Shorter Synthesis Time, Compared To Current Conventional Synthesis Methods. The Methods Reduce The Total Number Of Steps In The Synthesis From Four To Five Down To Two, Thereby Simplifying Production; And Allow A Reduced Number Of Solvents And Reagents To Be Used In Production, Thereby Reducing The Waste Generated In The Synthesis. The Methods Can Reduce The Waste To About 3-5 Kilograms Of Waste Generated Per Kilogram Of Product Produced; And Surprisingly Improve The Overall Yield From 60-65% To Greater Than 90% As Compared To The Current Conventional Synthesis Methods For Amodiaquine And Its Analogs.
合成参考文献
参考文献:10.1016/j.chroma.2006.09.066 摘要:Lindegårdh N, Giorgi F, Galletti B, Di Mattia M, Quaglia M, Carnevale D, White NJ, Mazzanti A, Day NP. Identification of an isomer impurity in piperaquine drug substance. J Chromatogr A. 2006 Dec 01;1135(2):166–9. doi: 10.1016/j.chroma.2006.09.066.