Nerisopam, EGIS-6775, GYKI-52322
奈立索泮Chemical Name: 1-(4-Aminophenyl)-4-methyl-7,8-dimethoxy-5H-2,3-benzodiazepine
CAS No. 102771-12-0, 102771-15-3 (diHCl), 102771-14-2 (monoHCl), 102771-16-4 (sulfate)
项目整合开发状态: Phase I
项目研究机构: Egis (Originator), Japan Tobacco (Licensee)
合成路线:1-(3,4-Dimethoxyphenyl)-2-propanol (I) is condensed with 4-nitrobenzaldehyde.The resulting 1-(4-nitrophenyl)-3-methyl-6,7-dimethoxyisochromane (II) is oxidized with Jones reagent to obtain 2-acetonyl-4,5-dimethoxy-4'-nitrobenzophenone (III).Then 1-(4-nitrophenyl)-3-methyl-6,7-dimethoxy-2-benzopyrylium perchlorate (IV) is produced by the conventional procedure,from which intermediary,with the help of hydrazine hydrate and reduction.GYKI-52322 is prepared.
📌 参考资料/链接：
参考文献标题:5H-2,3-Benzodiazepine derivs.and pharmaceutical c
文献作者:Lang,T.; Kori,J.; Andr醩i,F.; Botka,P.; H醡ori,T.; Berzsenyi,P.; Goldschmidt,K.; Z髄yomi,G.; Elekes,I.; L醤g,Z.(Egis Pharmaceuticals Ltd.)
参考来源:BE 0902953; CH 667090; DE 3527117; ES 8608494; FR 2568252; GB 2162184; JP 1986043174; US 4614740
📄 详细内容
合成路线:1-(3,4-Dimethoxyphenyl)-2-propanol (I) is condensed with 4-nitrobenzaldehyde.The resulting 1-(4-nitrophenyl)-3-methyl-6,7-dimethoxyisochromane (II) is oxidized with Jones reagent to obtain 2-acetonyl-4,5-dimethoxy-4'-nitrobenzophenone (III).Then 1-(4-nitrophenyl)-3-methyl-6,7-dimethoxy-2-benzopyrylium perchlorate (IV) is produced by the conventional procedure,from which intermediary,with the help of hydrazine hydrate and reduction.GYKI-52322 is prepared.
参考文献标题:Process for preparing isochromane derivs.
文献作者:Hamori,T.; Botka,P.; Zolyomi,G.; Koeroesi,J.; Lang,T.(Gyogyszerkutato Intezet Kft.)
参考来源:HU 194550
合成路线:1-(3,4-Dimethoxyphenyl)-2-propanol (I) is condensed with 4-nitrobenzaldehyde.The resulting 1-(4-nitrophenyl)-3-methyl-6,7-dimethoxyisochromane (II) is oxidized with Jones reagent to obtain 2-acetonyl-4,5-dimethoxy-4'-nitrobenzophenone (III).Then 1-(4-nitrophenyl)-3-methyl-6,7-dimethoxy-2-benzopyrylium perchlorate (IV) is produced by the conventional procedure,from which intermediary,with the help of hydrazine hydrate and reduction.GYKI-52322 is prepared.
参考文献标题:New process for producing 2-aroyl-phenylacetone derivs.
文献作者:Somogyi,G.; Balogh,T.; Botka,P.; Lang,T.; Hamori,T.; Zolyomi,G.; Koeroesi,J.(Gyogyszerkutato Intezet Kft.)
参考来源:HU 194529
合成路线:1-(3,4-Dimethoxyphenyl)-2-propanol (I) is condensed with 4-nitrobenzaldehyde.The resulting 1-(4-nitrophenyl)-3-methyl-6,7-dimethoxyisochromane (II) is oxidized with Jones reagent to obtain 2-acetonyl-4,5-dimethoxy-4'-nitrobenzophenone (III).Then 1-(4-nitrophenyl)-3-methyl-6,7-dimethoxy-2-benzopyrylium perchlorate (IV) is produced by the conventional procedure,from which intermediary,with the help of hydrazine hydrate and reduction.GYKI-52322 is prepared.
参考文献标题:GYKI-52322
文献作者:Andr醩i,F.
参考来源:Drugs Fut 1988,13(4),308
产品链接: CAS No. 102771-12-0››