Namirotene, CBS-211A
那米罗汀Chemical Name: (E)-4-[2-(2-Isopropyl-5-thienyl)propenyl]benzoic acid
CAS No. 101506-83-6
项目整合开发状态: Phase I
项目研究机构: Chauvin (Originator)
合成路线:The addition of methyl magnesium iodide to 2-acetylthiophene (I) and subsequent reduction of the propenyl derivative (II) with H2 over Pd/C in methanol yields the 2-isopropylthiophene (III),which is acetylated with acetyl chloride.Reduction of 2-isopropyl-5-acetylthiophene (IV) with lithium aluminum hydride gives the corresponding alcohol,which is converted to the triphenylphosphonium salt (V).By Wittig reaction with 4-ethoxycarbonyl benzaldehyde (VI) the ethyl ester obtained is then hydrolyzed with potassium hydroxide to yield the free acid.
📌 参考资料/链接：
参考文献标题:New derivatives of 4-vinyl benzoic acid,process for their preparation and their uses in therapeutics ans as ligands
文献作者:Coquelet,C.; Roussillon,S.; Sincholle,D.; Bonne,C.; Alazet,A.(Chauvin Laboratories SA)
参考来源:EP 0161156; FR 8405531; US 4929635; WO 8504652
📄 详细内容
合成路线:The addition of methyl magnesium iodide to 2-acetylthiophene (I) and subsequent reduction of the propenyl derivative (II) with H2 over Pd/C in methanol yields the 2-isopropylthiophene (III),which is acetylated with acetyl chloride.Reduction of 2-isopropyl-5-acetylthiophene (IV) with lithium aluminum hydride gives the corresponding alcohol,which is converted to the triphenylphosphonium salt (V).By Wittig reaction with 4-ethoxycarbonyl benzaldehyde (VI) the ethyl ester obtained is then hydrolyzed with potassium hydroxide to yield the free acid.
参考文献标题:CBS-211 A
文献作者:Bonne,C.; Conduzorgues,J.P.; Coquelet,C.; Roussillon,S.
参考来源:Drugs Fut 1986,11(7),557
产品链接: CAS No. 101506-83-6››