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【结 构 式】 
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【分子编号】35581 【品名】(2R)-2-([[4-(4-bromophenoxy)phenyl]sulfonyl]amino)-3,3-dimethylbutyric acid 【CA登记号】 |
【 分 子 式 】C18H20BrNO5S 【 分 子 量 】442.33054 【元素组成】C 48.88% H 4.56% Br 18.06% N 3.17% O 18.09% S 7.25% |
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：(IV)Chlorosulfonation of 4-bromodiphenyl ether (I) in cold CH2Cl2 afforded the corresponding sulfonyl chloride (II). After silylation of D-tert-leucine (III) with chlorotrimethylsilane and N-methylmopholine, coupling with acid chloride (II) provided sulfonamide (IV). Conversion of (IV) to acid chloride (V) was then achieved by treatment with oxalyl chloride and a catalytic amount of DMF at low temperature. Finally, condensation of (V) with hydroxylamine in aqueous THF gave rise to the target hydroxamic acid.
| 【1】 Abreo, M.A.; Bender, S.L. (Agouron Pharmaceuticals, Inc.); Metalloproteinase inhibitors, pharmaceutical compsns. containing them and their pharmaceutical uses. EP 0973748; WO 9843963 . |
| 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) | 35580 | 1-bromo-4-phenoxybenzene; 4-bromophenyl phenyl ether | 101-55-3 | C12H9BrO | 详情 | 详情 |
| (II) | 35579 | 4-(4-bromophenoxy)benzenesulfonyl chloride | C12H8BrClO3S | 详情 | 详情 | |
| (III) | 35583 | (2R)-2-amino-3,3-dimethylbutyric acid; D-tert-Leucine | 26782-71-8 | C6H13NO2 | 详情 | 详情 |
| (IV) | 35581 | (2R)-2-([[4-(4-bromophenoxy)phenyl]sulfonyl]amino)-3,3-dimethylbutyric acid | C18H20BrNO5S | 详情 | 详情 | |
| (V) | 35582 | (2R)-2-([[4-(4-bromophenoxy)phenyl]sulfonyl]amino)-3,3-dimethylbutanoyl chloride | C18H19BrClNO4S | 详情 | 详情 |
Extended Information