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CAS 114772-54-2
4'-(bromomethyl)-[1,1'-biphenyl]-2-carbonitrile
登记编号:TELM-029、OLME-011、IRBE-004、ALIS-008、VALS-001、AZILS-017、AZIL-004、CAND-004
应用背景(按来源药适应症)
高血压替米沙坦/苯磺酸氨氯地平/氢氯噻嗪高血压瑞舒伐他汀钙/替米沙坦高脂血症瑞舒伐他汀钙/替米沙坦高血压奥美沙坦酯/马来酸氨氯地平高血压Olmesartan Medoxomil/Amlodipine orotate高血压Atorvastatin Calcium Hydrate/Irbesartan高脂血症Atorvastatin Calcium Hydrate/Irbesartan高血压阿利沙坦酯高血压苯磺酸左旋氨氯地平/缬沙坦原发性高血压苯磺酸左旋氨氯地平/缬沙坦原发性高血压缬沙坦/氨氯地平乳清酸盐原发性高血压缬沙坦/盐酸乐卡地平高血压厄贝沙坦/三氯噻嗪高血压阿齐沙坦原发性高血压阿齐沙坦二型糖尿病阿齐沙坦肥胖症阿齐沙坦糖尿病阿齐沙坦高血压阿齐沙坦酯钾盐/氯噻酮原发性高血压阿齐沙坦酯钾盐/氯噻酮高血压苯磺酸氨氯地平/坎地沙坦酯高血压奥美沙坦酯/阿折地平高血压苯磺酸氨氯地平/替米沙坦原发性高血压苯磺酸氨氯地平/奥美沙坦酯高血压苯磺酸氨氯地平/奥美沙坦酯高血压奥美沙坦酯缺血性卒中奥美沙坦酯心脏衰竭奥美沙坦酯代谢综合征奥美沙坦酯肾小球肾炎奥美沙坦酯二型糖尿病奥美沙坦酯高血压替米沙坦乳腺癌替米沙坦心肌疾病替米沙坦阿尔茨海默病替米沙坦风险降低手段替米沙坦心肌梗塞替米沙坦左心室功能不全缬沙坦高血压缬沙坦原发性高血压缬沙坦肺动脉高压缬沙坦右心室功能障碍缬沙坦心肌梗塞后综合征缬沙坦食道疾病厄贝沙坦高血压厄贝沙坦糖尿病肾病厄贝沙坦高胆固醇血症厄贝沙坦白蛋白尿厄贝沙坦二型糖尿病厄贝沙坦原发性高血压美阿沙坦钾高血压美阿沙坦钾高血压坎地沙坦西酯心脏衰竭坎地沙坦西酯原发性高血压坎地沙坦西酯偏头痛坎地沙坦西酯新型冠状病毒感染坎地沙坦西酯躁狂症坎地沙坦西酯
来源药(使用该中间体的合成路线)
| 品种 | 梯队 | 到期年 |
|---|---|---|
| 替米沙坦/苯磺酸氨氯地平/氢氯噻嗪Telmisartan/Amlodipine Besylate/Hydrochlorothiazide | Tier C · 观察 / 贸易 | - |
| 瑞舒伐他汀钙/替米沙坦Rosuvastatin Calcium/Telmisartan | Tier C · 观察 / 贸易 | - |
| 奥美沙坦酯/马来酸氨氯地平Olmesartan Medoxomil/Amlodipine Maleate | Tier C · 观察 / 贸易 | - |
| Olmesartan Medoxomil/Amlodipine orotate | Tier C · 观察 / 贸易 | - |
| Atorvastatin Calcium Hydrate/Irbesartan | Tier C · 观察 / 贸易 | - |
| 阿利沙坦酯Allisartan Isoproxil | Tier C · 观察 / 贸易 | - |
| 苯磺酸左旋氨氯地平/缬沙坦Levamlodipine Besylate/Valsartan | Tier C · 观察 / 贸易 | - |
| 缬沙坦/氨氯地平乳清酸盐Valsartan/Amlodipine Orotate | Tier C · 观察 / 贸易 | - |
| 缬沙坦/盐酸乐卡地平Valsartan/Lercanidipine Hydrochloride | Tier C · 观察 / 贸易 | - |
| 厄贝沙坦/三氯噻嗪Irbesartan/Trichlormethiazide | Tier C · 观察 / 贸易 | - |
| 阿齐沙坦Azilsartan | Tier C · 观察 / 贸易 | - |
| 阿齐沙坦酯钾盐/氯噻酮Azilsartan Medoxomil Potassium/Chlorthalidone | Tier C · 观察 / 贸易 | - |
| 苯磺酸氨氯地平/坎地沙坦酯Amlodipine Besylate/Candesartan Cilexetil | Tier C · 观察 / 贸易 | - |
| 奥美沙坦酯/阿折地平Olmesartan Medoxomil/Azelnidipine | Tier C · 观察 / 贸易 | - |
| 苯磺酸氨氯地平/替米沙坦Amlodipine Besylate/Telmisartan | Tier C · 观察 / 贸易 | - |
| 苯磺酸氨氯地平/奥美沙坦酯Amlodipine Besylate/Olmesartan Medoxomil | Tier C · 观察 / 贸易 | - |
| 奥美沙坦酯Olmesartan Medoxomil | Tier B · 提前布局 | - |
| 替米沙坦Telmisartan | Tier B · 提前布局 | - |
| 缬沙坦Valsartan | Tier B · 提前布局 | - |
| 厄贝沙坦Irbesartan | Tier B · 提前布局 | - |
| 美阿沙坦钾Azilsartan Medoxomil Potassium | Tier C · 观察 / 贸易 | - |
| 坎地沙坦西酯Candesartan Cilexetil | Tier B · 提前布局 | - |
合成路线中的位置(上下游链)
按路线登记顺序排列,左→右为合成方向;高亮为当前 CAS,其余可点击跳转对应档案。
diethyl 2-propyl-1H-imidazole-4,5-dicarboxylate→ethyl 4-(2-hydroxypropan-2-yl)-2-propyl-1H-imidazole-5-carboxylate→4-(chloromethyl)-5-methyl-1,3-dioxol-2-one→(5-methyl-2-oxo-1,3-dioxol-4-yl)methyl 4-(2-hydroxypropan-2-yl)-2-propyl-1-((2'-(1-trityl-1H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-1H-imidazole-5-carboxylate→4'-(bromomethyl)-[1,1'-biphenyl]-2-carbonitrile→ethyl 1-((2'-cyano-[1,1'-biphenyl]-4-yl)methyl)-4-(2-hydroxypropan-2-yl)-2-propyl-1H-imidazole-5-carboxylate→1-((2'-(1H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-4-(2-hydroxypropan-2-yl)-2-propyl-1H-imidazole-5-carboxylic acid
4-(chloromethyl)-5-methyl-1,3-dioxol-2-one→4'-(bromomethyl)-[1,1'-biphenyl]-2-carbonitrile→4-(2-hydroxypropan-2-yl)-2-propyl-1H-imidazole-5-carbonitrile→4,4-dimethyl-2-propyl-4,6-dihydro-1H-furo[3,4-d]imidazol-6-ol→4'-((6-hydroxy-4,4-dimethyl-2-propyl-4,6-dihydro-1H-furo[3,4-d]imidazol-1-yl)methyl)-[1,1'-biphenyl]-2-carbonitrile→1-((2'-cyano-[1,1'-biphenyl]-4-yl)methyl)-4-(2-hydroxypropan-2-yl)-2-propyl-1H-imidazole-5-carboxylic acid→(5-methyl-2-oxo-1,3-dioxol-4-yl)methyl 1-((2'-cyano-[1,1'-biphenyl]-4-yl)methyl)-4-(2-hydroxypropan-2-yl)-2-propyl-1H-imidazole-5-carboxylate
diethyl 2-propyl-1H-imidazole-4,5-dicarboxylate→ethyl 4-(2-hydroxypropan-2-yl)-2-propyl-1H-imidazole-5-carboxylate→4-(chloromethyl)-5-methyl-1,3-dioxol-2-one→(5-methyl-2-oxo-1,3-dioxol-4-yl)methyl 4-(2-hydroxypropan-2-yl)-2-propyl-1-((2'-(1-trityl-1H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-1H-imidazole-5-carboxylate→4'-(bromomethyl)-[1,1'-biphenyl]-2-carbonitrile→ethyl 1-((2'-cyano-[1,1'-biphenyl]-4-yl)methyl)-4-(2-hydroxypropan-2-yl)-2-propyl-1H-imidazole-5-carboxylate→1-((2'-(1H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-4-(2-hydroxypropan-2-yl)-2-propyl-1H-imidazole-5-carboxylic acid
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