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CAS 589-15-1

1-bromo-4-(bromomethyl)benzene

登记编号：OLME-016、IRBE-013、VALS-012、CAND-034

应用背景（按来源药适应症）

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/三氯噻嗪高血压苯磺酸氨氯地平/坎地沙坦酯高血压奥美沙坦酯/阿折地平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

来源药（使用该中间体的合成路线）

品种梯队到期年
奥美沙坦酯/马来酸氨氯地平Olmesartan Medoxomil/Amlodipine MaleateTier C · 观察 / 贸易-
Olmesartan Medoxomil/Amlodipine orotateOlmesartan Medoxomil/Amlodipine orotateTier C · 观察 / 贸易-
Atorvastatin Calcium Hydrate/IrbesartanAtorvastatin Calcium Hydrate/IrbesartanTier C · 观察 / 贸易-
苯磺酸左旋氨氯地平/缬沙坦Levamlodipine Besylate/ValsartanTier C · 观察 / 贸易-
缬沙坦/氨氯地平乳清酸盐Valsartan/Amlodipine OrotateTier C · 观察 / 贸易-
缬沙坦/盐酸乐卡地平Valsartan/Lercanidipine HydrochlorideTier C · 观察 / 贸易-
厄贝沙坦/三氯噻嗪Irbesartan/TrichlormethiazideTier C · 观察 / 贸易-
苯磺酸氨氯地平/坎地沙坦酯Amlodipine Besylate/Candesartan CilexetilTier C · 观察 / 贸易-
奥美沙坦酯/阿折地平Olmesartan Medoxomil/AzelnidipineTier C · 观察 / 贸易-
苯磺酸氨氯地平/奥美沙坦酯Amlodipine Besylate/Olmesartan MedoxomilTier C · 观察 / 贸易-

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。

奥美沙坦酯/马来酸氨氯地平优化路线步数：5总收率：40 mg
ethyl 4-(2-hydroxypropan-2-yl)-2-propyl-1H-imidazole-5-carboxylate→4-(chloromethyl)-5-methyl-1,3-dioxol-2-one→1-bromo-4-(bromomethyl)benzene→ethyl 1-(4-bromobenzyl)-4-(2-hydroxypropan-2-yl)-2-propyl-1H-imidazole-5-carboxylate→(2-(1-(2-phenylpropan-2-yl)-1H-tetrazol-5-yl)phenyl)boronic acid→ethyl 4-(2-hydroxypropan-2-yl)-1-((2'-(1-(2-phenylpropan-2-yl)-1H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-2-propyl-1H-imidazole-5-carboxylate→4-(2-hydroxypropan-2-yl)-1-((2'-(1-(2-phenylpropan-2-yl)-1H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-2-propyl-1H-imidazole-5-carboxylic acid→(5-methyl-2-oxo-1,3-dioxol-4-yl)methyl 4-(2-hydroxypropan-2-yl)-1-((2'-(1-(2-phenylpropan-2-yl)-1H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-2-propyl-1H-imidazole-5-carboxylate
Olmesartan Medoxomil/Amlodipine orotate优化路线步数：5总收率：40 mg
ethyl 4-(2-hydroxypropan-2-yl)-2-propyl-1H-imidazole-5-carboxylate→4-(chloromethyl)-5-methyl-1,3-dioxol-2-one→1-bromo-4-(bromomethyl)benzene→ethyl 1-(4-bromobenzyl)-4-(2-hydroxypropan-2-yl)-2-propyl-1H-imidazole-5-carboxylate→(2-(1-(2-phenylpropan-2-yl)-1H-tetrazol-5-yl)phenyl)boronic acid→ethyl 4-(2-hydroxypropan-2-yl)-1-((2'-(1-(2-phenylpropan-2-yl)-1H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-2-propyl-1H-imidazole-5-carboxylate→4-(2-hydroxypropan-2-yl)-1-((2'-(1-(2-phenylpropan-2-yl)-1H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-2-propyl-1H-imidazole-5-carboxylic acid→(5-methyl-2-oxo-1,3-dioxol-4-yl)methyl 4-(2-hydroxypropan-2-yl)-1-((2'-(1-(2-phenylpropan-2-yl)-1H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-2-propyl-1H-imidazole-5-carboxylate
Atorvastatin Calcium Hydrate/Irbesartan优化路线步数：5总收率：380.00 mg
1,4-dibromobenzene→4-bromobenzaldehyde→(4-bromophenyl)methanol→1-bromo-4-(bromomethyl)benzene→2-butyl-1,3-diazaspiro[4.4]non-1-en-4-one hydrochloride→3-(4-bromobenzyl)-2-butyl-1,3-diazaspiro[4.4]non-1-en-4-one→(2-(1-trityl-1H-tetrazol-5-yl)phenyl)boronic acid
苯磺酸左旋氨氯地平/缬沙坦优化路线步数：3总收率：/
methyl L-valinate hydrochloride→pentanoyl chloride→1-bromo-4-(bromomethyl)benzene→(S)-methyl 2-((4-bromobenzyl)amino)-3-methylbutanoate→(S)-methyl 2-(N-(4-bromobenzyl)pentanamido)-3-methylbutanoate→(2-(1-trityl-1H-tetrazol-5-yl)phenyl)boronic acid→(S)-methyl 3-methyl-2-(N-((2'-(1-trityl-1H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)pentanamido)butanoate
缬沙坦/氨氯地平乳清酸盐优化路线步数：3总收率：/
methyl L-valinate hydrochloride→pentanoyl chloride→1-bromo-4-(bromomethyl)benzene→(S)-methyl 2-((4-bromobenzyl)amino)-3-methylbutanoate→(S)-methyl 2-(N-(4-bromobenzyl)pentanamido)-3-methylbutanoate→(2-(1-trityl-1H-tetrazol-5-yl)phenyl)boronic acid→(S)-methyl 3-methyl-2-(N-((2'-(1-trityl-1H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)pentanamido)butanoate
缬沙坦/盐酸乐卡地平优化路线步数：3总收率：/
methyl L-valinate hydrochloride→pentanoyl chloride→1-bromo-4-(bromomethyl)benzene→(S)-methyl 2-((4-bromobenzyl)amino)-3-methylbutanoate→(S)-methyl 2-(N-(4-bromobenzyl)pentanamido)-3-methylbutanoate→(2-(1-trityl-1H-tetrazol-5-yl)phenyl)boronic acid→(S)-methyl 3-methyl-2-(N-((2'-(1-trityl-1H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)pentanamido)butanoate
厄贝沙坦/三氯噻嗪优化路线步数：5总收率：380.00 mg
1,4-dibromobenzene→4-bromobenzaldehyde→(4-bromophenyl)methanol→1-bromo-4-(bromomethyl)benzene→2-butyl-1,3-diazaspiro[4.4]non-1-en-4-one hydrochloride→3-(4-bromobenzyl)-2-butyl-1,3-diazaspiro[4.4]non-1-en-4-one→(2-(1-trityl-1H-tetrazol-5-yl)phenyl)boronic acid
苯磺酸氨氯地平/坎地沙坦酯优化路线步数：15总收率：2.05 g
3-nitrophthalic acid→triethoxymethoxyethane→cyclohexyl (1-iodoethyl) carbonate→1-(((cyclohexyloxy)carbonyl)oxy)ethyl 2-ethoxy-1-((2'-(1-trityl-1H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-1H-benzo[d]imidazole-7-carboxylate→2-(methoxycarbonyl)-6-nitrobenzoic acid→methyl 2-(chlorocarbonyl)-3-nitrobenzoate→methyl 2-(azidocarbonyl)-3-nitrobenzoate→methyl 2-((tert-butoxycarbonyl)amino)-3-nitrobenzoate→1-bromo-4-(bromomethyl)benzene→methyl 2-((4-bromobenzyl)(tert-butoxycarbonyl)amino)-3-nitrobenzoate→methyl 2-((4-bromobenzyl)amino)-3-nitrobenzoate→methyl 3-amino-2-((4-bromobenzyl)amino)benzoate→methyl 1-(4-bromobenzyl)-2-ethoxy-1H-benzo[d]imidazole-7-carboxylate→1-(4-bromobenzyl)-2-ethoxy-1H-benzo[d]imidazole-7-carboxylic acid→1-(((cyclohexyloxy)carbonyl)oxy)ethyl 1-(4-bromobenzyl)-2-ethoxy-1H-benzo[d]imidazole-7-carboxylate→(2-(1-trityl-1H-tetrazol-5-yl)phenyl)boronic acid→benzonitrile→5-phenyl-2H-tetrazole→5-phenyl-1-trityl-1H-tetrazole
奥美沙坦酯/阿折地平优化路线步数：5总收率：40 mg
ethyl 4-(2-hydroxypropan-2-yl)-2-propyl-1H-imidazole-5-carboxylate→4-(chloromethyl)-5-methyl-1,3-dioxol-2-one→1-bromo-4-(bromomethyl)benzene→ethyl 1-(4-bromobenzyl)-4-(2-hydroxypropan-2-yl)-2-propyl-1H-imidazole-5-carboxylate→(2-(1-(2-phenylpropan-2-yl)-1H-tetrazol-5-yl)phenyl)boronic acid→ethyl 4-(2-hydroxypropan-2-yl)-1-((2'-(1-(2-phenylpropan-2-yl)-1H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-2-propyl-1H-imidazole-5-carboxylate→4-(2-hydroxypropan-2-yl)-1-((2'-(1-(2-phenylpropan-2-yl)-1H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-2-propyl-1H-imidazole-5-carboxylic acid→(5-methyl-2-oxo-1,3-dioxol-4-yl)methyl 4-(2-hydroxypropan-2-yl)-1-((2'-(1-(2-phenylpropan-2-yl)-1H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-2-propyl-1H-imidazole-5-carboxylate
苯磺酸氨氯地平/奥美沙坦酯优化路线步数：5总收率：40 mg
ethyl 4-(2-hydroxypropan-2-yl)-2-propyl-1H-imidazole-5-carboxylate→4-(chloromethyl)-5-methyl-1,3-dioxol-2-one→1-bromo-4-(bromomethyl)benzene→ethyl 1-(4-bromobenzyl)-4-(2-hydroxypropan-2-yl)-2-propyl-1H-imidazole-5-carboxylate→(2-(1-(2-phenylpropan-2-yl)-1H-tetrazol-5-yl)phenyl)boronic acid→ethyl 4-(2-hydroxypropan-2-yl)-1-((2'-(1-(2-phenylpropan-2-yl)-1H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-2-propyl-1H-imidazole-5-carboxylate→4-(2-hydroxypropan-2-yl)-1-((2'-(1-(2-phenylpropan-2-yl)-1H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-2-propyl-1H-imidazole-5-carboxylic acid→(5-methyl-2-oxo-1,3-dioxol-4-yl)methyl 4-(2-hydroxypropan-2-yl)-1-((2'-(1-(2-phenylpropan-2-yl)-1H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-2-propyl-1H-imidazole-5-carboxylate

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