【药物名称】CI-933
化学结构式(Chemical Structure):
参考文献No.184
标题:1-Aroyl-5-oxo-2-pyrrolidinepropanoic acid derivs.
作者:(Pfizer Inc.)
来源:EP 0110575; ES 8600238
合成路线图解说明:

The partial hydrolysis of perhydropyrrolizine-3,5-dione (I) in the presence of benzyl alcohol (II) by means of aqueous concentrated HCl at 98 C gives benzyl 5-oxopyrrolidine-2-propenoate (III), which is condensed with 4-methoxybenzoyl chloride (IV) by means of triethylamine in hot THF to afford benzyl 1-(4-methoxybenzoyl)-5-oxopyrrolidine-3-propanoate (V). Finally, this compound ls debenzylated by hydrogenolysis with H2 over Pd/C in THF.

参考文献No.49801
标题:CI-933
作者:Casta馿r, J.; Serradell, M.N.
来源:Drugs Fut 1985,10(12),972
合成路线图解说明:

The partial hydrolysis of perhydropyrrolizine-3,5-dione (I) in the presence of benzyl alcohol (II) by means of aqueous concentrated HCl at 98 C gives benzyl 5-oxopyrrolidine-2-propenoate (III), which is condensed with 4-methoxybenzoyl chloride (IV) by means of triethylamine in hot THF to afford benzyl 1-(4-methoxybenzoyl)-5-oxopyrrolidine-3-propanoate (V). Finally, this compound ls debenzylated by hydrogenolysis with H2 over Pd/C in THF.

参考文献No.546824
标题:Synthesis of carbon-14 labeled 1-(4-methoxybenzoyl
作者:Huang, C.C.
来源:J Label Compd Radiopharm 1987,24(6),675
合成路线图解说明:

The esterification of bromoacetic acid (I) with benzyl alcohol (II) gives the corresponding ester (III), which by reaction with triphenylphosphine (IV) in hot toluene yields the phosphonium bromide (V). The reaction of (V) with NaOH in water-dichloromethane affords benzyl(triphenylphosphoranylidene) acetate (VI), which is submitted to a Wittig condensation with 5-(hydroxymethyl)-2-pyrrolidone (VII) in the presence of Dess-Martin periodinane (DMPI) giving benzyl 3-(5-oxo-2-pyrrolidinyl)-2(E) propenoate (VIII). The acylation of (VIII) with 4-methoxybenzoyl chloride (IX) by means of triethylamine in hot toluene yields the corresponding amide (X), which is finally hydrogenated and deprotected with H2 over Pd/C in THF.

Drug Information Express,Drug R&D,Chemical Database,Patent Search.
Copyright © 2006-2024 Drug Future. All rights reserved.Contact Us