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枸橼酸托瑞米芬的中间体合成工艺改进 被引量:4

Improvement on the synthesis of an intermediate for toremifene citrate
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摘要 目的:研究了抗肿瘤药物枸橼酸托瑞米芬的中间体1,2-二苯基-1-[4-[2-(N,N-二甲胺基)乙氧苯基]]-1,4-丁二醇的合成工艺改进。方法:以4-羟基二苯甲酮为原料经过取代与加成两步反应合成了目标物,并进行工艺的优化实验。结果:中间体合成工艺得到改进和优化,两步收率合计55.4%。结论:研究出了一条生产成本低,反应温和,操作简单的枸橼酸托瑞米芬的中间体合成工艺。 Objective: To synthesize a key intermediate of antineoplastic drug, 1,2--dibenzyl--1--[4--[-2- (N, N - dimethylamino) ethoxyl-] phenyl] -- butane -- 1,4 -- diol. Methods : The intermediate was synthesized with 4--hydroxydiphenyl ketone as raw materials, by substitution reaction and addition reaction. Results:The intermediate has been optimized and improved. The overall yield is 55.4 ~. Conclusion:The mild and easy syn- thesis process, which has a lower cost, has been worked out.
出处 《黑龙江医药科学》 2012年第4期29-30,共2页 Heilongjiang Medicine and Pharmacy
关键词 1 2-二苯基-1-[4-[2-(N N-二甲氨基)乙氧苯基]]-1 4-丁二醇 肉桂醇 托瑞米芬 抗肿瘤药物 1,2 - dibenzyl - 1 - [4 -- [-2 - (N, N - dimethylamino) ethoxyl-]phenyl-] - butane - 1,4 - diol cinnamyl alcohol toremifene citrate antineoplastic
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