【结 构 式】 |
【药物名称】Haloxazolam, CS-430, Somelin 【化学名称】10-Bromo-11b-(2-fluorophenyl)-2,3,5,6,7,11b-hexahydro[1,3]oxazolo[3,2-d][1,4]benzodiazepin-6-one 【CA登记号】59128-97-1 【 分 子 式 】C17H14BrFN2O2 【 分 子 量 】377.21573 |
【开发单位】Sankyo (Originator) 【药理作用】PSYCHOPHARMACOLOGIC DRUGS, Sedative/Hypnotics, Sleep Disorders, Treatment of |
合成路线1
By reaction of 2-aminobenzophenones (I) with bromoacetyl halide (II) or tosyloxyacetyl halide (VI) to give, respectively, 2-(bromoacetylamino)benzophenones (III) or 2-(tosyloxyacetylamino)benzophenones (VII), which are treated with ethanolamine (IV) to give the compounds (V), which with acetic acid in ethanol give the desired compounds. These compounds can also be obtained from (III) and (VI) without isolation of (V)
【1】 Miyadera, T.; et al.; J Heterocycl Chem 1973, 10, 6, 85-88. |
【2】 Shishoo, C.J.; et al.; Process for the manufacture of pharmacologically active new heterocyclic compounds and salts thereof. IN 151496 . |
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) | 60640 | (2-amino-5-bromophenyl)(2-fluorophenyl)methanone | C13H9BrFNO | 详情 | 详情 | |
(II) | 27903 | 2-Bromoacetyl chloride | 22118-09-8 | C2H2BrClO | 详情 | 详情 |
(III) | 60641 | 2-bromo-N-[4-bromo-2-(2-fluorobenzoyl)phenyl]acetamide | C15H10Br2FNO2 | 详情 | 详情 | |
(IV) | 10259 | Ethanol amine;Ethanolamine;2-Aminoethanol; 2-Amino-1-ethanol;2-Aminoethyl alcohol | 141-43-5 | C2H7NO | 详情 | 详情 |
(V) | 60642 | N-[4-bromo-2-(2-fluorobenzoyl)phenyl]-2-[(2-hydroxyethyl)amino]acetamide | C17H16BrFN2O3 | 详情 | 详情 | |
(VI) | 60643 | 2-chloro-2-oxoethyl 4-methylbenzenesulfonate | C9H9ClO4S | 详情 | 详情 | |
(VII) | 60644 | 2-[4-bromo-2-(2-fluorobenzoyl)anilino]-2-oxoethyl 4-methylbenzenesulfonate | C22H17BrFNO5S | 详情 | 详情 |
Extended Information