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【结 构 式】 
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【分子编号】15875 【品名】[2-[2-(tert-butyl)-2H-1,2,3,4-tetraazol-5-yl]phenyl](chloro)zinc 【CA登记号】 |
【 分 子 式 】C11H13ClN4Zn 【 分 子 量 】302.09388 【元素组成】C 43.74% H 4.34% Cl 11.74% N 18.55% Zn 21.65% |
合成路线1
该中间体在本合成路线中的序号：(XI)3) The 8-[2'-(2-tert-butyltetrazol-5-yl)biphenyl-4-ylmethyl]-2,4-dimethyl-5,6,7,8-tetrahydropyrido[2,3-d]pyrimidin-7-one (VIII) can also be obtained as follows: The reaction of the previously described 5-(2-bromophenyl)-2-tertbutyltetrazole (X) with Mg in THF catalyzed with 1,2-dibromoethane gives the corresponding Grignard reagent, which is treated with ZnCl2 yielding the organozinc derivative (XI). Finally, this compound is condensed with the previously described intermediate 8-(4-bromobenzyl)-2,4-dimethyl-5,6,7,8-tetrahydropyrido-[2,3-d]pyrimidin-7-one (VI) catalyzed by bis(triphenylphosphine)palladium and diisobutylaluminum hydride in THF.
| 【1】 Merlos, M.; Casas, A.; Castaner, J.; Tasosartan. Drugs Fut 1997, 22, 8, 850. |
| 【2】 Giguere, P.; Iera, S.; Bernatchez, M.; Barreca, G.; Castaldi, G.; Cannata, V. (American Home Products Corp.); Process for preparation of biphenyl derivs. WO 9640684 . |
| 中间体序号 | 中间体编号 | 品名 | CAS号 | 分子式 | 供应商 | 用于合成 |
|---|---|---|---|---|---|---|
| (VI) | 15870 | 8-(4-bromobenzyl)-2,4-dimethyl-5,8-dihydropyrido[2,3-d]pyrimidin-7(6H)-one | C16H16BrN3O | 详情 | 详情 | |
| (VIII) | 15872 | 8-([2'-[2-(tert-butyl)-2H-1,2,3,4-tetraazol-5-yl][1,1'-biphenyl]-4-yl]methyl)-2,4-dimethyl-5,8-dihydropyrido[2,3-d]pyrimidin-7(6H)-one | C27H29N7O | 详情 | 详情 | |
| (X) | 15874 | 5-(2-bromophenyl)-2-(tert-butyl)-2H-1,2,3,4-tetraazole | C11H13BrN4 | 详情 | 详情 | |
| (XI) | 15875 | [2-[2-(tert-butyl)-2H-1,2,3,4-tetraazol-5-yl]phenyl](chloro)zinc | C11H13ClN4Zn | 详情 | 详情 |