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【结 构 式】 
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【分子编号】58104 【品名】1-propylpiperazine 【CA登记号】 |
【 分 子 式 】C7H16N2 【 分 子 量 】128.21752 【元素组成】C 65.57% H 12.58% N 21.85% |
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：(V)The mono-silylation of 2-aminoresorcinol (I) by means of tert-butyldimethylsilyl chloride and triethylamine yields silyl ether (II). Condensation of rifamycin S (III) with aminophenol (II), followed by oxidative treatment with MnO2 produces the benzoxazinorifamycin derivative (IV). Addition of N-propyl piperazine (V) to (IV) in the presence of MnO2 leads to the target piperazinyl benzoxazinorifamycin.
| 【1】 Yamashita, K.; Yamane, T.; Sakashita, S.; Hosoe, K.; Fujii, K. (Kaneka Corp.); Remedy for diseases caused by infection with Helicobacter. EP 0787494; EP 0861660; JP 1998298080; US 5981522; WO 9709047 . |
| 【2】 Yamane, T.; et al.; Synthesis and biological activity of 3'-hydroxy-5'-aminobenzoxazinorifamycin derivatives. Chem Pharm Bull 1993, 41, 1, 148. |
| 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) | 58101 | 2-amino-1,3-benzenediol | C6H7NO2 | 详情 | 详情 | |
| (II) | 58102 | 2-amino-3-{[tert-butyl(dimethyl)silyl]oxy}phenol | C12H21NO2Si | 详情 | 详情 | |
| (III) | 31943 | Rifamycin S; (7S,11S,12R,13S,14R,15R,16R,17S,18S)-2,15,17-trihydroxy-11-methoxy-3,7,12,14,16,18,22-heptamethyl-6,23,27,29-tetraoxo-8,30-dioxa-24-azatetracyclo[23.3.1.1(4,7).0(5,28)]triaconta-1(28),2,4,9,19,21,25-heptaen-13-yl acetate | C37H45NO12 | 详情 | 详情 | |
| (IV) | 58103 | (7S,11S,12R,13S,14R,15R,16R,17S,18S)-32-{[tert-butyl(dimethyl)silyl]oxy}-2,15,17-trihydroxy-11-methoxy-3,7,12,14,16,18,22-heptamethyl-6,23,37-trioxo-8,27,38-trioxa-24,34-diazahexacyclo[23.11.1.1~4,7~.0~5,36~.0~26,35~.0~28,33~]octatriaconta-1(36),2,4 | C49H62N2O13Si | 详情 | 详情 | |
| (V) | 58104 | 1-propylpiperazine | C7H16N2 | 详情 | 详情 |
Extended Information