发明名称 PROCESS FOR THE PREPARATION OF HIGHLY PURE HYDROXYCHLOROQUINE OR A SALT THEREOF
摘要 The present invention is directed at a process for selectively removing compound of formula 1 or a salt thereof from a mixture comprising compound of formula I and compound of formula 4: see formula 4 wherein the process comprises the steps of: (i) putting the mixture in solution and treating the solution with a reactant selected from the group consisting of: see formula (A) where X is halogen, OH or OCOR'; Hal is halogen; Y is O or S; W is O, N or S; and R, R', and R" are each independently selected from the group consisting of alkyl, aryl, and aralkyl; to yield protected compounds of formula 5 and diprotected compounds of formula 6, see formula 6 said protected compounds of formula 5 and diprotected compounds of formula 6 being soluble in the solution; (ii) hydrolysis, in a suitable solvent, of the protected compounds of formula 5 and the diprotected compounds of formula 6 by using a metal hydroxide or metal carbonate, to yield soluble compounds of formula 1 and soluble protected compounds of formula 7; see formula 7 (iii) adding an acid, preferably sulfuric acid, to form an insoluble salt of compounds of formula 1; (iv) isolating the insoluble salt of compound of formula 1; and optionally, recovering the compound of formula 1 from its salt.
申请公布号 CA2561987(A1) 申请公布日期 2008.04.02
申请号 CA20062561987 申请日期 2006.10.02
申请人 APOTEX PHARMACHEM INC. 发明人 DUNCAN, SAMMY CHRIS;GUNTOORI, BHASKAR REDDY;CHE, DAQING;MONTEMAYOR, LAURA KAYE
分类号 C07D215/46 主分类号 C07D215/46
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