Dabelotine mesilate, S-12024-2
(±)-1-甲基-8-(吗啡烯-2-甲氧基)-1,2,3,4-四氢喹啉甲烷磺酸盐 达贝洛汀 Chemical Name: (?-1-Methyl-8-(morpholin-2-ylmethoxy)-1,2,3,4-tetrahydroquinoline methanesulfonate
CAS No. 153049-48-0, 118976-38-8 (free base)
项目整合开发状态: Phase III
项目研究机构: ADIR (Originator), Servier (Originator)
合成路线:The condensation of 4-benzyl-2-(chloromethyl)morpholine (I) with 8-hydroxy-1,2,3,4-tetrahydroquinoline (II) by means of NaH in hot DMF gives 8-(4-benzylmorpholin-2-ylmethoxy)-1,2,3,4-tetrahydroquinoline (III),which is methylated with methyl iodide and K2CO3 in refluxing acetone yielding the corresponding N-methyl derivative (IV).Finally,this compound is debenzylated by hydrogenolysis with H2 over Pd/C in ethanol.
📌 参考资料/链接：
参考文献标题:Novel morpholine derivs.,process for their preparation and pharmaceutical compsns.containing them
文献作者:R間nier,G.; Guillonneau,C.; Lepagnol,J.(ADIR et Cie.)
参考来源:AU 8813520; EP 0286495; FR 2612926; JP 1988255279; US 4782054
📄 详细内容
合成路线:The condensation of 4-benzyl-2-(chloromethyl)morpholine (I) with 8-hydroxy-1,2,3,4-tetrahydroquinoline (II) by means of NaH in hot DMF gives 8-(4-benzylmorpholin-2-ylmethoxy)-1,2,3,4-tetrahydroquinoline (III),which is methylated with methyl iodide and K2CO3 in refluxing acetone yielding the corresponding N-methyl derivative (IV).Finally,this compound is debenzylated by hydrogenolysis with H2 over Pd/C in ethanol.
参考文献标题:Dabelotine Mesylate
文献作者:Tracy,M.; Ngo,J.; Castar,J.
参考来源:Drugs Fut 1996,21(9),890
产品链接: CAS No. 153049-48-0›› 产品链接: CAS No.118976-38-8››