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Lotrifen, L-12717, DL-717IT, Privaprol, Canocenta

氯曲芬Chemical Name: 2-(4-Chlorophenyl)[1,2,4]triazolo[5,1-a]isoquinoline
CAS No. 66535-86-2
项目整合开发状态: Registered
项目研究机构: Altana Pharma (Originator), Lepetit (Originator)
合成路线:By cyclization of 2-amino-3,4-dihydro-1(2H)-isoquinolinone (I) with m-ethoxybenzimidic acid ethyl ester (II) at 125 C.

合成路线:The cyclization of 2-amino-3,4-dihydro-1(2H)-isoquinolinone (I) with ethyl 4-chlorobenzimidate (II) by heating at 125 C under vacuum gives 2-(4-chloro-phenyl)-5,6-dihydro-s-triazolo[5,1-a]isoquinoline (III),which is dehydrogenated by means of N-bromoacetamide in refluxing CCl4.
📌 参考资料/链接:
参考文献标题:2-Substd.phenyl-5-triazols[5,1-a]isoquinoline cpds
文献作者:Consonni,P.; Lerner,L.; Omodei-Sal? A.(Lepetit SpA)
参考来源:US 4075341

📄 详细内容


合成路线:The condensation of 2-amino-1(2H)-isoquinolinone (IV) with imidate (II) by heating at 125 C as before gives 2-(4-cholorobenzimidoylamino)-1(2H)-isoquinolinone (V),which is cyclized by means of NaH in ethoxyethanol.

参考文献标题:S-triazolo[5,1-a]isochinolin derivate
文献作者:Omodai-Sale,A.; Consonni,P.; Lerner,L.(Lepetit SpA)
参考来源:DE 2707272; NL 7704940


合成路线:By cyclization of isoquinolinone (IV) with 4-chlorobenzonitrile (VI) by means of sodium ethoxide in refluxing ethanol.

参考文献标题:Triazolo[5,1-a]isoquinoline deriv
文献作者:Omodei-Sale,A.; Favara,D.(Lepetit SpA)
参考来源:DE 2942195; FR 2440369


合成路线:The cyclization of 2-amino-3,4-dihydro-1(2H)-isoquinolinone (I) with ethyl 4-chlorobenzimidate (II) by heating at 125 C under vacuum gives 2-(4-chloro-phenyl)-5,6-dihydro-s-triazolo[5,1-a]isoquinoline (III),which is dehydrogenated by means of N-bromoacetamide in refluxing CCl4.

合成路线:By cyclization of isoquinolinone (IV) with 4-chlorobenzonitrile (VI) by means of sodium ethoxide in refluxing ethanol.

合成路线:The condensation of 2-amino-1(2H)-isoquinolinone (IV) with imidate (II) by heating at 125 C as before gives 2-(4-cholorobenzimidoylamino)-1(2H)-isoquinolinone (V),which is cyclized by means of NaH in ethoxyethanol.
参考文献标题:Lotrifen
文献作者:de Angelis,L.; Castar,J.
参考来源:Drugs Fut 1985,10(10),817


产品链接: CAS No. 66535-86-2››