【结 构 式】 |
【分子编号】65810 【品名】N-Methylphenylacetohydroxamic Acid; N-Hydroxy-N-Methyl-2-Phenyl-Acetamide; N-Hydroxy-N-Methyl-2-Phenyl-Ethanamide 【CA登记号】72229-75-5 |
【 分 子 式 】C9H11NO2 【 分 子 量 】165.19188 【元素组成】C 65.44% H 6.71% N 8.48% O 19.37% |
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 bromo amide intermediate (XI) is prepared by condensation of phenylacetyl chloride (XIII) with N-methylhydroxylamine hydrochloride in the presence of Et3N in CH2Cl2 to produce the Weinreb amide (XIV), which is then acylated with methanesulfonyl chloride and Et3N followed by ultrasound-promoted rearrangement of the N-sulfonyloxy amide intermediate in the presence of DIEA and LiBr in acetonitrile (1). Scheme 2.
【1】 Weller, T., Koberstein, R., Aissaoui, H., Clozel, M., Fischli, W. (Actelion Pharmaceuticals Ltd.). Substituted 1,2,3,4-tetrahydroisoquinoline derivatives. EP 1751111, JP 2007525531, US 2007191424, WO 2005118548. |
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) | 65808 | 2-Bromo-N-Methyl-2-Phenyl-Acetamide | 51685-62-2 | C9H10BrNO | 详情 | 详情 |
(XIII) | 25890 | 2-phenylacetyl chloride;Phenylacetyl chloride;Phenacetyl chloride;Benzeneacetyl chloride | 103-80-0 | C8H7ClO | 详情 | 详情 |
(XIV) | 65810 | N-Methylphenylacetohydroxamic Acid; N-Hydroxy-N-Methyl-2-Phenyl-Acetamide; N-Hydroxy-N-Methyl-2-Phenyl-Ethanamide | 72229-75-5 | C9H11NO2 | 详情 | 详情 |
Extended Information