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【结 构 式】

【分子编号】33728

【品名】2-phenylsuccinic acid

【CA登记号】635-51-8

【 分 子 式 】C10H10O4

【 分 子 量 】194.187

【元素组成】C 61.85% H 5.19% O 32.96%

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:(XIV)

The reaction of 6,7,8,9-tetrahydronaphtho[1,2-d][1,3]dioxol-6-one (I) with nitromethane by means of butylamine in refluxing toluene/methylcyclohexane/acetic acid gives the nitromethyl derivative (XIII), which is reduced with H2 over Pd/C in methanol to yield the previously described amine (VII). Amine (VII) can be condensed with 2-phenylsuccinic acid by means of acetyl chloride in refluxing xylene yielding directly the previously reported succinimide (X) as a mixture of the cis and trans racemic diastereomers.

1 Deshpande, M.N.; et al.; A scalable process for the novel antidepressant ABT-200. Org Process Res Dev 1998, 2, 6, 351.
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) 33715 8,9-dihydronaphtho[1,2-d][1,3]dioxol-6(7H)-one C11H10O3 详情 详情
(VII) 33724 6,7,8,9-tetrahydronaphtho[1,2-d][1,3]dioxol-6-ylmethylamine; 6,7,8,9-tetrahydronaphtho[1,2-d][1,3]dioxol-6-ylmethanamine C12H15NO2 详情 详情
(X) 33722 3-phenyl-1-(6,7,8,9-tetrahydronaphtho[1,2-d][1,3]dioxol-6-ylmethyl)-2,5-pyrrolidinedione C22H21NO4 详情 详情
(XII) 33726 6-[(E)-nitromethylidene]-6,7,8,9-tetrahydronaphtho[1,2-d][1,3]dioxole C12H11NO4 详情 详情
(XIII) 33727 6-(nitromethyl)-8,9-dihydronaphtho[1,2-d][1,3]dioxole C12H11NO4 详情 详情
(XIV) 33728 2-phenylsuccinic acid 635-51-8 C10H10O4 详情 详情
Extended Information