Nomifensine maleate, Hoe-984, Merital
诺米芬新马来酸盐 诺米芬辛 Chemical Name: 8-Amino-2-methyl-4-phenyl-1,2,3,4-tetrahydroisoquinoline maleate
CAS No. 32795-47-4, 24526-64-5 (free base)
项目整合开发状态: Launched
项目研究机构: Aventis Pharma (Originator)
合成路线:By condensation of 2-nitrobenzylmethylamine (I) with alpha-bromoacetophenone (A) in ethanol to give omega-[N-(2-nitrobenzyl)methylamino]acetophenone (II) (HCl salt,m.p.165-7 C),which is then reduced first with H2 over Pd/C,or Ni-diatomaceous earth and afterwards with NaBH4 in CH2Cl2 to give N-(2-aminobenzyl)-1-phenyl-2-methylaminoethanol (III),m.p.67-9 C.This product is finally cyclized with sulfuric acid.
📌 参考资料/链接：
参考文献标题:4-Phenyl-8-amino tetrahydroisoquinolines
文献作者:Hoffmann,I.; Gustav,E.; Heinrich,O.; Schmitt,K.(Aventis Pharma AG)
参考来源:DE 1670694; DE 1670848; FR 1524487; FR 6496M; FR 6646M; GB 1164192; US 3577424
📄 详细内容
合成路线:By condensation of 2-nitrobenzylmethylamine (I) with alpha-bromoacetophenone (A) in ethanol to give omega-[N-(2-nitrobenzyl)methylamino]acetophenone (II) (HCl salt,m.p.165-7 C),which is then reduced first with H2 over Pd/C,or Ni-diatomaceous earth and afterwards with NaBH4 in CH2Cl2 to give N-(2-aminobenzyl)-1-phenyl-2-methylaminoethanol (III),m.p.67-9 C.This product is finally cyclized with sulfuric acid.
参考文献标题:8-Amino-4-phenyl-1,2,3,4-tetrahydroisoquinolines,a new group of anti-depressive psycholeptic drugs
文献作者:Hoffmann,I.; Gustav,E.; Schmitt,K.
参考来源:Arzneim-Forsch Drug Res 1971,21(7),1045
合成路线:By condensation of 2-nitrobenzylmethylamine (I) with alpha-bromoacetophenone (A) in ethanol to give omega-[N-(2-nitrobenzyl)methylamino]acetophenone (II) (HCl salt,m.p.165-7 C),which is then reduced first with H2 over Pd/C,or Ni-diatomaceous earth and afterwards with NaBH4 in CH2Cl2 to give N-(2-aminobenzyl)-1-phenyl-2-methylaminoethanol (III),m.p.67-9 C.This product is finally cyclized with sulfuric acid.
参考文献标题:Nomifensin
文献作者:Chatterjee,S.S.; Castar,J.
参考来源:Drugs Fut 1976,1(2),72
产品链接: CAS No. 32795-47-4›› 产品链接: CAS No.24526-64-5››