【结 构 式】 |
【分子编号】46875 【品名】tert-butyl 5-methoxy-2-nitrophenyl(methyl)carbamate 【CA登记号】 |
【 分 子 式 】C13H18N2O5 【 分 子 量 】282.2964 【元素组成】C 55.31% H 6.43% N 9.92% O 28.34% |
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:(IV)The intermediate phenylenediamine (VI) was prepared as follows. Reaction of 5-chloro-2-nitroaniline (I) with sodium methoxide afforded 5-methoxy-2-nitroaniline (II), which was subsequently converted to the N-Boc derivative (III). Methylation of (III) with iodomethane and NaH, followed by acidic treatment of the resulting N-methyl carbamate (IV), produced the N-methyl aniline (V). The nitro group of (V) was then reduced with the combination SnCl2-NaBH4 to furnish the diamine (VI).
【1】 Fujita, T.; Wada, K.; Oguchi, M.; Yanagisawa, H.; Fujimoto, K.; Fujiwara, T.; Horikoshi, H.; Yoshioka, T. (Sankyo Co., Ltd.); Benzimidazole derivs., their preparation and their therapeutic use. CA 2177858; EP 0745600; JP 1997295970; JP 2000001487; US 5886014 . |
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) | 15709 | 5-chloro-2-nitrophenylamine; 5-chloro-2-nitroaniline | 1635-61-6 | C6H5ClN2O2 | 详情 | 详情 |
(II) | 42920 | 5-methoxy-2-nitrophenylamine; 5-methoxy-2-nitroaniline | 16133-49-6 | C7H8N2O3 | 详情 | 详情 |
(III) | 46874 | tert-butyl 5-methoxy-2-nitrophenylcarbamate | C12H16N2O5 | 详情 | 详情 | |
(IV) | 46875 | tert-butyl 5-methoxy-2-nitrophenyl(methyl)carbamate | C13H18N2O5 | 详情 | 详情 | |
(V) | 46876 | 5-methoxy-N-methyl-2-nitroaniline; N-(5-methoxy-2-nitrophenyl)-N-methylamine | C8H10N2O3 | 详情 | 详情 | |
(VI) | 46877 | N-(2-amino-5-methoxyphenyl)-N-methylamine; 4-methoxy-N(2)-methyl-1,2-benzenediamine | C8H12N2O | 详情 | 详情 |
Extended Information