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氟康唑合成新工艺研究.pdf

发布:2015-09-03约6.9千字共3页下载文档
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王健祥(, 225300) : 改进氟康唑( fluconzole 1)的合成工艺 用间二氟苯为起始原料, 用 4氨基1H1, 2, 4三氮唑代替 1H1, 2, 4三氮唑,分别采用 转移催化和超声波方法, 经三步反应制得氟康唑 得氟康唑 ( 1), mp137~ 141 , 总收率 50% 符合中国药典 2000年版二部的标准, 工艺可靠, 质量稳定 : 氟康唑; 转移; 合成;超声波 : TQ464. 4 : : 2006) Study on the new preparation of fluconazole W NG Jianxiang(Ta izhou P oly tech n ical Institute J iang su, Ta izhou 225300, Ch ina) ABSTRACT: OBJECTIVE To mi prove the synthesis technology of fluconazole. MET ODS F luconazolewas prepared after three steps reaction with mdifluorobenzenes as starting material and 1H1, 2, 4triazole was replaced by 4am ino1H1, 2, 4triazole. The phase transfer catalysis and ultrasonicmethod have been adopted separately in this technology. RESULTS The melting point of the productwas in the range of 137 and 141 and the overall yield was 50%. CONCLUSION ccording to the pharmacopoeia of People s Republic ofChine standard, the technology is reliable and the quality is stable. KEY WORDS: fluconazole; phase transfer; preparation; ultrasonic ( fluconzole 1) 2( 2, 4 )1, 3 ( 1H1, 2, 41) 2, 1 [1] , , 1983( Pfizer) [2] , , ,, 1992 ,, [ 1] ( FriedelCrafts) 1H1, 2, 4, N1, [ 56] , ,, 0~ 5 N4 , , [ 7] 40~ 50 ; , 3~ 10% , ( 3), 90% 1H1, 2, 4, ( 3) [ 34] ( 4), ,
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