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【结 构 式】

【分子编号】29831

【品名】benzyl 3-[1-(4-methoxybenzoyl)-5-oxo-2-pyrrolidinyl]propanoate

【CA登记号】

【 分 子 式 】C22H23NO5

【 分 子 量 】381.42836

【元素组成】C 69.28% H 6.08% N 3.67% O 20.97%

与该中间体有关的原料药合成路线共 1 条

合成路线1

该中间体在本合成路线中的序号:(V)

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.

1 (Pfizer Inc.); 1-Aroyl-5-oxo-2-pyrrolidinepropanoic acid derivs.. EP 0110575; ES 8600238 .
2 Castaner, J.; Serradell, M.N.; CI-933. Drugs Fut 1985, 10, 12, 972.
中间体序号 中间体编号 品名 CAS号 分子式 供应商 用于合成
(I) 29829 dihydro-1H-pyrrolizine-3,5(2H,6H)-dione C7H9NO2 详情 详情
(II) 18710 Benzyl alcohol; Phenylmethanol 100-51-6 C7H8O 详情 详情
(III) 29830 benzyl 3-(5-oxo-2-pyrrolidinyl)propanoate C14H17NO3 详情 详情
(IV) 22671 4-Methoxybenzoyl chloride; p-Methoxybenzoyl chloride; 4-Anisoyl chloride 100-07-2 C8H7ClO2 详情 详情
(V) 29831 benzyl 3-[1-(4-methoxybenzoyl)-5-oxo-2-pyrrolidinyl]propanoate C22H23NO5 详情 详情
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