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盐酸氯卡色林消旋体的合成工艺改进 被引量:3

Improvement the Synthesis Process of Lorcaserin Hydrochloride Racemate
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摘要 改进盐酸氯卡色林消旋体的合成工艺,以对氯苯乙腈为起始原料,经还原得到中间体对氯苯乙胺,与2-氯丙酰氯反应,再经傅克烷基化反应成环,然后使用硼氢化钠、三氯化铝还原体系还原酰胺,最后成盐,得到目标产物,总收率达25.0%。 This study is to synthesize lorcaserin hydrochloride racemate and improve the process. The 4-chlorophenethylamine was synthesized from 4-chlorobenzyl cyanide by reduction, and then it was reacted with 2-chloropropionyl chloride, through cyclization, reduction by sodium borohydride and aluminum chloride,finally through salt formation, to form lorcaserin hydrochloride racemate, with an overall yield of 25.0%.
出处 《药学与临床研究》 2014年第3期237-238,共2页 Pharmaceutical and Clinical Research
关键词 盐酸氯卡色林消旋体 合成 减肥药 Lorcaserin hydrochloride racemate Synthesis Antiobesity agent
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参考文献4

  • 1Aytes S, Sengupta D, Smith B, et al. Processes for pre- paring 3-benzazepines: WO, 2005019179[P]. 2005-03-03.
  • 2Gharbaoui T, Tandel SK, Carlos M, et al. Processes for preparing (R)-8-chloro-l-methyl-2,3,4,5 -tetrahydro - 1H -3 -benzazepine and intermediates thereof: WO, 2008070111[P]. 2008-06-12.
  • 3Ulrich W, Frank P, Christoph S, et al. Processes for the preparation of 8-chl, oro-l-methyl-2,3,4,5-tctrahy- dro-lH-3-benzazepine and intermediates related there- to: US, 20090143576[P]. 2009-06-04.
  • 4汪迅,李新涓子,李勇刚,等.氯卡色林盐酸盐的制备方法:CN103333111A[P].2013-10-02.

共引文献3

同被引文献41

  • 1汪迅,李新涓子,李勇刚,等.氯卡色林盐酸盐的制备方法:CN103333111A[P].2013-10-02.
  • 2Smith J,Smith B.5HT2C receptor modulators:WO,2003086306[P].2003-10-23.
  • 3Behan DP,Smith BM,Bjenning C.5HT2C receptor modulatorcompositions and methods of use:WO,2006071740[P].2006-07-06.
  • 4Smith BM,Smith JM,Tsai JH,et al.Discovery and structureactivityrelationship of (1R)-8-chloro-2,3,4,5-tetrahydro-1-methyl-1H-3-benzazepine (Lorcaserin),a selective serotonin HT2C receptor agonist for the treatment of obesity[J].JMed Chem,2008,51(2):305-313.
  • 5Smith B,Gilson C,Schultz J,et al.Benzazepine derivativesand methods of prophylaxis or treatment of 5HT2C receptorassociated diseases:WO,2005042491[P].2005-05-12.
  • 6Smith B,Schultz J,Gilson C,et al.Benzazepine derivativesand methods of prophylaxis or treatment of 5HT2C receptorassociateddiseases:WO,2005042490[P].2005-05-12.
  • 7Zhu QH,Wang JW,Bian XG,et al.Novel synthesis ofantiobesity drug lorcaserin hydrochloride[J].Org Proc ResDev,2015,19(9):1263-1267.
  • 8Duranlópez E.Process for the enantioselective synthesis ofa tetrahydrobenzazepine compound:WO,2014060575[P].2014-04-24.
  • 9何爱民.1-(苯乙基氨基)丙烷-2-醇类化合物或其盐的制备方法:中国,103601645[P].2014-02-26.
  • 10Smith B,Gilson C,Schultz J,et al.Benzazepine derivativesuseful for the treatment of 5HT2C receptor associateddiseases:WO,2005003096[P].2005-01-13.

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