FS-205-397
6-乙氧基-3,3-二甲基-1,2-二氢吲哚甲烷磺酸盐 6-乙氧基-3,3-二甲基-1,2-二氢吲哚 Chemical Name: 6-Ethoxy-3,3-dimethyl-2,3-dihydro-1H-indole methanesulfonate; 6-Ethoxy-3,3-dimethylindoline methanesulfonate
CAS No. 116861-51-9, 87234-87-5 (free base)
项目整合开发状态: Phase II
项目研究机构: Novartis (Originator)
合成路线:FS-205-397 can be obtained by two related ways:1) The acetylation of 6-ethoxyindolin-2-one (I) with refluxing acetic anhydride gives 1-acetyl-6-ethoxyindolin-2-one (II),which is methylated with methyliodide and butyllithium in HMPT to yield 6-ethoxy-3,3-dimethylindolin-2-one (III).Finally,this compound is reduced with LiAlH4 in THF.2) The acetylation of 6-hydroxyindolin-2-one (IV) with refluxing acetic anhydride gives 6-acetoxy-1-acetylindolin-2-one (V),which is methylated as before,affording 6-hydroxy-3,3-dimethylindolin-2-one (VI).Finally,this compound is ethylated with ethyl iodide and K2CO3 in refluxing acetone to give the indolinone (III),already obtained.
📌 参考资料/链接：
参考文献标题:3,3-Dialkyl and 3,3-alkylene-indoline derivs.,process for their preparation and pharmaceutical compsns.Containing them
文献作者:Achini,R.(Novartis Deutschland GmbH)
参考来源:DE 3300522
📄 详细内容
合成路线:FS-205-397 can be obtained by two related ways:1) The acetylation of 6-ethoxyindolin-2-one (I) with refluxing acetic anhydride gives 1-acetyl-6-ethoxyindolin-2-one (II),which is methylated with methyliodide and butyllithium in HMPT to yield 6-ethoxy-3,3-dimethylindolin-2-one (III).Finally,this compound is reduced with LiAlH4 in THF.2) The acetylation of 6-hydroxyindolin-2-one (IV) with refluxing acetic anhydride gives 6-acetoxy-1-acetylindolin-2-one (V),which is methylated as before,affording 6-hydroxy-3,3-dimethylindolin-2-one (VI).Finally,this compound is ethylated with ethyl iodide and K2CO3 in refluxing acetone to give the indolinone (III),already obtained.
参考文献标题:FS-205-397
文献作者:Castar,J.; Prous,J.
参考来源:Drugs Fut 1992,17(3),185
产品链接: CAS No. 116861-51-9›› 产品链接: CAS No.87234-87-5››