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【结 构 式】 
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【分子编号】58918 【品名】4-[(4-{3-[(4R)-4-methyl-2,5-dioxo-3-phenylimidazolidinyl]propoxy}phenyl)sulfonyl]tetrahydro-2H-pyran-4-carboxylic acid 【CA登记号】 |
【 分 子 式 】C25H28N2O8S 【 分 子 量 】516.572 【元素组成】C 58.13% H 5.46% N 5.42% O 24.78% S 6.21% |
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：(XIII)N-Arylation of hydantoin (XI) with phenylboronic acid in the presence of cupric acetate gives rise to the N-phenyl hydantoin (XII). Subsequent hydrolysis of the tert-butyl ester with trifluoroacetic acid in CH2Cl2 affords acid (XIII). This is then coupled with O-(tetrahydropyranyl)-hydroxylamine, yielding the tetrahydropyranyl-protected hydroxamic acid (XIV). Finally, removal of the tetrahydropyranyl protecting group of (XIV) under acidic conditions provides the title compound.
| 【1】 Becker, D.P.; Villamil, C.; Barta, T.E.; et al.; Design and synthesis of potent and selective 4,4-disubstituted alpha-sulphones hydroxamates as MMP inhibitors. 224th ACS Natl Meet (Aug 18 2002, Boston) 2002, Abst MEDI 309. |
| 中间体序号 | 中间体编号 | 品名 | CAS号 | 分子式 | 供应商 | 用于合成 |
|---|---|---|---|---|---|---|
| (XI) | 58916 | tert-butyl 4-[(4-{3-[(4R)-4-methyl-2,5-dioxoimidazolidinyl]propoxy}phenyl)sulfonyl]tetrahydro-2H-pyran-4-carboxylate | C23H32N2O8S | 详情 | 详情 | |
| (XII) | 58917 | tert-butyl 4-[(4-{3-[(4R)-4-methyl-2,5-dioxo-3-phenylimidazolidinyl]propoxy}phenyl)sulfonyl]tetrahydro-2H-pyran-4-carboxylate | C29H36N2O8S | 详情 | 详情 | |
| (XIII) | 58918 | 4-[(4-{3-[(4R)-4-methyl-2,5-dioxo-3-phenylimidazolidinyl]propoxy}phenyl)sulfonyl]tetrahydro-2H-pyran-4-carboxylic acid | C25H28N2O8S | 详情 | 详情 | |
| (XIV) | 58919 | 4-[(4-{3-[(4R)-4-methyl-2,5-dioxo-3-phenylimidazolidinyl]propoxy}phenyl)sulfonyl]-N-(tetrahydro-2H-pyran-2-yloxy)tetrahydro-2H-pyran-4-carboxamide | C30H37N3O9S | 详情 | 详情 |
Extended Information