【结 构 式】 |
【药物名称】 【化学名称】4-[4-(4-Chlorophenyl)-1H-pyrazol-3-yl]morpholine 【CA登记号】88743-53-7 【 分 子 式 】C13H14ClN3O 【 分 子 量 】263.72903 |
【开发单位】Asta Medica (Originator) 【药理作用】Antiepileptic Drugs, NEUROLOGIC DRUGS, Sodium Channel Blockers |
合成路线1
(4-Chlorophenyl)thioacetic acid morpholide (II) was prepared by Willgerodt-Kindler reaction of 4'-chloroacetophenone (I) with sulfur and morpholine. Subsequent condensation of (II) with triethyl orthoformate and morpholine provided the 3-(4-morpholinyl)thioacrylic acid morpholide (IIIa-b). Finally, ring closure of (IIIa-b) with hydrazine hydrochloride in refluxing EtOH furnished the title pyrazole.
【1】 Unverferth, K.; et al.; Synthesis, anticonvulsant activity, and structure-activity relationships of sodium channel blocking 3-aminopyrroles. J Med Chem 1998, 41, 1, 63. |
中间体序号 | 中间体编号 | 品名 | CAS号 | 分子式 | 供应商 | 用于合成 |
---|---|---|---|---|---|---|
(IIIa) | 32943 | (E)-2-(4-chlorophenyl)-1,3-di(4-morpholinyl)-2-propene-1-thione | C17H21ClN2O2S | 详情 | 详情 | |
(IIIb) | 32944 | (Z)-2-(4-chlorophenyl)-1,3-di(4-morpholinyl)-2-propene-1-thione | C17H21ClN2O2S | 详情 | 详情 | |
(I) | 12685 | 4-Chloroacetophenone; 1-(4-Chlorophenyl)-1-ethanone; p-Chloroacetophenone | 99-91-2 | C8H7ClO | 详情 | 详情 |
(II) | 32942 | 2-(4-chlorophenyl)-1-(4-morpholinyl)-1-ethanethione | C12H14ClNOS | 详情 | 详情 |
Extended Information