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【结 构 式】

【分子编号】64349

【品名】ethyl 1-{[2'-({(3,4-dimethyl-5-isoxazolyl)[(2-methoxyethoxy)methyl]amino}sulfonyl)-2-methyl[1,1'-biphenyl]-4-yl]methyl}-4-ethyl-2-propyl-1H-imidazole-5-carboxylate

【CA登记号】

【 分 子 式 】C34H44N4O7S

【 分 子 量 】652.81212

【元素组成】C 62.56% H 6.79% N 8.58% O 17.16% S 4.91%

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:(XI)

Mesylate (IX) is condensed with ethyl 2-propyl-4-ethylimidazole-5-carboxylate (X) yielding (XI). Simultaneous ester group hydrolysis and MEM group deprotection under acidic conditions gives rise to the imidazolecarboxylic acid (XII). This is finally coupled with methylamine via activation with CDI to produce the desired N-methyl carboxamide (1-3).

1 Tellew, J.E.; Baska, R.A.F.; Beyer, S.M.; Carlson, K.E.; Cornelius, L.A.; Fadnis, L.; Gu, Z..; Kunst, B.L.; Kowala, M.C.; Monshizadegan, H.; Murugesan, N.; Ryan, C.S.; Valentine, M.T.; Yang, Y.; Macor, J.E.; Discovery of 4'-[(Imidazol-1-yl)methyl]biphenyl-2-sulfonamides as dual endothelin/Angiotensin II receptor antagonists. Bioorg Med Chem Lett 2003, 13, 6, 1093.
2 Macor, J.E.; Murugesan, N.; Gu, Z.; Tellew, J.E. (Bristol-Myers Squibb Co.); Biphenyl sulfonamides as dual angiotensin endothelin receptor antagonists. EP 1094816; JP 2002519380; US 2002143024; WO 0001389 .
3 Macor, J.E.; Murugesan, N.; Gu, Z.; Tellew, J.E. (Bristol-Myers Squibb Co.); Biphenyl sulfonamides as dual angiotensin endothelin receptor antagonists. EP 1237888; WO 0144239 .
中间体序号 中间体编号 品名 CAS号 分子式 供应商 用于合成
(IX) 64347 [2'-({(3,4-dimethyl-5-isoxazolyl)[(2-methoxyethoxy)methyl]amino}sulfonyl)-2-methyl[1,1'-biphenyl]-4-yl]methyl methanesulfonate C24H30N2O8S2 详情 详情
(X) 64348 ethyl 4-ethyl-2-propyl-1H-imidazole-5-carboxylate C11H18N2O2 详情 详情
(XI) 64349 ethyl 1-{[2'-({(3,4-dimethyl-5-isoxazolyl)[(2-methoxyethoxy)methyl]amino}sulfonyl)-2-methyl[1,1'-biphenyl]-4-yl]methyl}-4-ethyl-2-propyl-1H-imidazole-5-carboxylate C34H44N4O7S 详情 详情
(XII) 64433 1-[(2'-{[(3,4-dimethyl-5-isoxazolyl)amino]sulfonyl}-2-methyl[1,1'-biphenyl]-4-yl)methyl]-4-ethyl-2-propyl-1H-imidazole-5-carboxylic acid C28H32N4O5S 详情 详情
Extended Information