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伊潘立酮的合成 被引量:10

Synthesis of Iloperidone
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摘要 (2,4-二氟苯基)-哌啶-4-基甲酮盐酸盐经肟化得到(2,4-二氟苯基)-哌啶-4-基甲酮肟盐酸盐,然后与4-(3-氯丙氧基)-3-甲氧基苯乙酮发生N-烷基化反应,再在氢氧化钾作用下闭环制得抗精神病药伊潘立酮,总收率约57%。 Iloperidone,an antipsychotic drug,was synthesized from(2,4-difluorophenyl)-piperidin-4- ylmethanone hydrochloride by oximination to give(2,4-difluorophenyl) -piperidin-4-ylmethanone oxime hydrochloride, followed by N-alkylation with 4-(3-chloropropoxy)-3-methoxyphenylethanone,and then cyclization in the presence of potassium hydroxide with an overall yield of about 57%.
出处 《中国医药工业杂志》 CAS CSCD 北大核心 2011年第2期88-89,95,共3页 Chinese Journal of Pharmaceuticals
关键词 伊潘立酮 抗精神病药 合成 ilopendone antipsychotic drug synthesis
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参考文献8

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二级参考文献3

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共引文献19

同被引文献52

  • 1段东红,康玉英,刘世斌.毛细管气相色谱法检测多潘立酮中的残留溶剂[J].药物分析杂志,2006,26(4):541-542. 被引量:1
  • 2陆学华,潘莉,唐承卓,程卯生.利培酮的合成[J].中国药物化学杂志,2007,17(2):89-91. 被引量:14
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  • 9郑立刚,尚振华,哈婧,等.伊潘立酮的制备方法:CN,20110226361.4[P].2013-02-13.
  • 10NGUYEN TB,BOUSSEROUEL H,WANG Q,et al.Chiral phosphoric acid-catalyzed enantioselectrive transfer hydrogenation of ortho-hydroxyaryl alkyl N-H ketimines[J].Org Lett,2010,12(20):4705-4707.

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