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CAS 103094-30-0,88150-62-3

3-Ethyl 5-methyl (4RS)-4-(2-chlorophenyl)-2-[[2-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)ethoxy]methyl]-6-methyl-1,4-dihydropyridine-3,5-dicarboxylate

登记编号:(VII)109067-2-a、Levamlodipine Besylate-011、(IX)109067-10-a

应用背景(按来源药适应症)

高血压Olmesartan Medoxomil/Amlodipine orotate原发性高血压缬沙坦/氨氯地平乳清酸盐高血压苯磺酸左旋氨氯地平心绞痛苯磺酸左旋氨氯地平原发性高血压苯磺酸左旋氨氯地平变异型心绞痛氨氯地平乳清酸盐高血压氨氯地平乳清酸盐缺血性心脏病氨氯地平乳清酸盐稳定型心绞痛氨氯地平乳清酸盐高血压樟脑磺酸氨氯地平高血压马来酸氨氯地平心绞痛马来酸氨氯地平慢性肾功能不全马来酸氨氯地平肾性高血压马来酸氨氯地平心脏病马来酸氨氯地平血管疾病马来酸氨氯地平

来源药(使用该中间体的合成路线)

品种梯队到期年
Olmesartan Medoxomil/Amlodipine orotateTier C · 观察 / 贸易-
缬沙坦/氨氯地平乳清酸盐Valsartan/Amlodipine OrotateTier C · 观察 / 贸易-
苯磺酸左旋氨氯地平Levamlodipine BesylateTier C · 观察 / 贸易-
氨氯地平乳清酸盐Amlodipine OrotateTier C · 观察 / 贸易-
樟脑磺酸氨氯地平Amlodipine CamsylateTier C · 观察 / 贸易-
马来酸氨氯地平Amlodipine MaleateTier 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。

Olmesartan Medoxomil/Amlodipine orotate优化路线步数:4总收率:/
Ethyl 4-chloro-3-oxobutanoate→Ethyl 4-[(4-methylbenzene-1-sulfonyl)oxy]-3-oxobutanoate→N-(2-Hydroxyethyl)phthalimide→Ethyl 4-(2-phthalimidoethoxy)acetoacetate→Ethyl (2Z)-3-amino-4-[2-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)ethoxy]but-2-enoate→Methyl (2Z)-2-[(2-chlorophenyl)methylidene]-3-oxobutanoate→3-Ethyl 5-methyl (4RS)-4-(2-chlorophenyl)-2-[[2-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)ethoxy]methyl]-6-methyl-1,4-dihydropyridine-3,5-dicarboxylate
缬沙坦/氨氯地平乳清酸盐优化路线步数:4总收率:/
Ethyl 4-chloro-3-oxobutanoate→Ethyl 4-[(4-methylbenzene-1-sulfonyl)oxy]-3-oxobutanoate→N-(2-Hydroxyethyl)phthalimide→Ethyl 4-(2-phthalimidoethoxy)acetoacetate→Ethyl (2Z)-3-amino-4-[2-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)ethoxy]but-2-enoate→Methyl (2Z)-2-[(2-chlorophenyl)methylidene]-3-oxobutanoate→3-Ethyl 5-methyl (4RS)-4-(2-chlorophenyl)-2-[[2-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)ethoxy]methyl]-6-methyl-1,4-dihydropyridine-3,5-dicarboxylate
氨氯地平乳清酸盐优化路线步数:4总收率:/
Ethyl 4-chloro-3-oxobutanoate→Ethyl 4-[(4-methylbenzene-1-sulfonyl)oxy]-3-oxobutanoate→N-(2-Hydroxyethyl)phthalimide→Ethyl 4-(2-phthalimidoethoxy)acetoacetate→Ethyl (2Z)-3-amino-4-[2-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)ethoxy]but-2-enoate→Methyl (2Z)-2-[(2-chlorophenyl)methylidene]-3-oxobutanoate→3-Ethyl 5-methyl (4RS)-4-(2-chlorophenyl)-2-[[2-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)ethoxy]methyl]-6-methyl-1,4-dihydropyridine-3,5-dicarboxylate
樟脑磺酸氨氯地平优化路线步数:4总收率:/
Ethyl 4-chloro-3-oxobutanoate→Ethyl 4-[(4-methylbenzene-1-sulfonyl)oxy]-3-oxobutanoate→N-(2-Hydroxyethyl)phthalimide→Ethyl 4-(2-phthalimidoethoxy)acetoacetate→Ethyl (2Z)-3-amino-4-[2-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)ethoxy]but-2-enoate→Methyl (2Z)-2-[(2-chlorophenyl)methylidene]-3-oxobutanoate→3-Ethyl 5-methyl (4RS)-4-(2-chlorophenyl)-2-[[2-(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)ethoxy]methyl]-6-methyl-1,4-dihydropyridine-3,5-dicarboxylate

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