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【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