Esonarimod, KE-298

2-乙酰基硫代甲基-3-(4-甲基苯甲酰)丙酸Chemical Name: (?-2-(Acetylsulfanylmethyl)-3-(4-methylbenzoyl)propionic acid; (?-2-(Acetylsulfanylmethyl)-4-(4-methylphenyl)-4-oxobutyric acid
CAS No. 101973-77-7
项目整合开发状态: Phase III
项目研究机构: Taisho (Originator)
合成路线:The Friedel-Crafts condensation of toluene (I) with itaconic anhydride (2-methylenesuccinic anhydride) (II) by means of AlCl3 in methylene chloride or 1,2-dichloroethane gives 3-(4-methylbenzoyl)-2-methylenepropionic acid (III),which is then treated with thioacetic acid (IV) and K2CO3 in DMF/water.
📌 参考资料/链接:
参考文献标题:Benzoylpropionic acid derivs.,their use and pharmaceutical compsns
文献作者:Tomisawa,K.; Kameo,K.; Matsunaga,T.; Saito,S.; Sota,K.(Taisho Pharmaceutical Co.,Ltd.)
参考来源:EP 0164101; ES 8603818; JP 1985258160

📄 详细内容


合成路线:The Friedel-Crafts condensation of toluene (I) with itaconic anhydride (2-methylenesuccinic anhydride) (II) by means of AlCl3 in methylene chloride or 1,2-dichloroethane gives 3-(4-methylbenzoyl)-2-methylenepropionic acid (III),which is then treated with thioacetic acid (IV) and K2CO3 in DMF/water.

参考文献标题:2-Acylthiomethyl-3-benzoylpropionic acid derivs
文献作者:Tomisawa,K.; Kameo,K.; Matsunaga,Y.; Saito,H.; Sodu,H.(Taisho Pharmaceutical Co.,Ltd.)
参考来源:JP 1987132825


合成路线:The Friedel-Crafts condensation of toluene (I) with itaconic anhydride (2-methylenesuccinic anhydride) (II) by means of AlCl3 in methylene chloride or 1,2-dichloroethane gives 3-(4-methylbenzoyl)-2-methylenepropionic acid (III),which is then treated with thioacetic acid (IV) and K2CO3 in DMF/water.

参考文献标题:Studies on antirheumatic agents: 3-Benzoylpropionic acid derivatives
文献作者:Kameo,K.; Ogawa,K.; Takeshita,K.; Nakaike,S.; Tomisawa,K.; Sota,K.
参考来源:Chem Pharm Bull 1988,36(6),2050-60


合成路线:The Friedel-Crafts condensation of toluene (I) with itaconic anhydride (2-methylenesuccinic anhydride) (II) by means of AlCl3 in methylene chloride or 1,2-dichloroethane gives 3-(4-methylbenzoyl)-2-methylenepropionic acid (III),which is then treated with thioacetic acid (IV) and K2CO3 in DMF/water.

参考文献标题:KE-298
文献作者:Mealy,N.; Castar,J.
参考来源:Drugs Fut 1996,21(7),691


合成路线:The Friedel-Crafts condensation of toluene (I) with itaconic anhydride (2-methylenesuccinic anhydride) (II) by means of AlCl3 in methylene chloride or 1,2-dichloroethane gives 3-(4-methylbenzoyl)-2-methylenepropionic acid (III),which is then treated with thioacetic acid (IV) and K2CO3 in DMF/water.
参考文献标题:A practical procedure for the synthesis of esonarimod,(R,S)-2-acetylthiomethyl-4-(4-methylphenyl)-4-oxobutanoic acid,an antirheumatic agent (Part 1)
文献作者:Noguchi,T.; Onodera,A.; Tomisawa,K.; Yokomori,S.
参考来源:Chem Pharm Bull 2002,50(10),1407


产品链接: CAS No. 101973-77-7››