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CAS 87269-87-2

Benzyl (2S,3aS,6aS)-octahydrocyclopenta[b]pyrrole-2-carboxylate hydrochloride

登记编号:Ramipril-008

应用背景(按来源药适应症)

高胆固醇血症阿托伐他汀钙/雷米普利高血压阿托伐他汀钙/雷米普利

来源药(使用该中间体的合成路线)

品种梯队到期年
阿托伐他汀钙/雷米普利Atorvastatin Calcium Hydrate/RamiprilTier 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。

阿托伐他汀钙/雷米普利工艺路线步数:7总收率:18.5kg(Ramipril (Free))
1-(1-Cyclopentenyl)pyrrolidine→(+/-)-Methyl 2-(Acetylamino)-3-chloropropionate→(Methyl 2-(acetylamino)-3-(2-oxocyclopentyl)propanoate)→(2S,3aS,6aS)-Octahydrocyclopenta[b]pyrrole-2-carboxylic acid hydrochloride→Benzyl (2S,3aR,6aS)-octahydrocyclopenta[b]pyrrole-2-carboxylic acid hydrochloride→N-[(S)-(+)-1-(Ethoxycarbonyl)-3-phenylpropyl]-L-alanine→(2S,3aS,6aS)-1-[N-[1(S)-(Ethoxycarbonyl)-3-phenylpropyl]-L-alanyl]perhydrocyclopenta[b]pyrrole-2-carboxylic acid→Benzyl (2S,3aS,6aS)-octahydrocyclopenta[b]pyrrole-2-carboxylate hydrochloride→Benzyl (2S,3aS,6aS)-octahydrocyclopenta[b]pyrrole-2-carboxylate sulfate
阿托伐他汀钙/雷米普利优化路线步数:2总收率:/
Benzyl (2S,3aS,6aS)-octahydrocyclopenta[b]pyrrole-2-carboxylate→Benzyl (2S,3aS,6aS)-octahydrocyclopenta[b]pyrrole-2-carboxylate hydrochloride→Ethyl (2S)-2-[(4S)-4-methyl-2,5-dioxo-1,3-oxazolidin-3-yl]-4-phenylbutanoate→(2S,3aS,6aS)-1-[N-[1(S)-(Ethoxycarbonyl)-3-phenylpropyl]-L-alanyl]perhydrocyclopenta[b]pyrrole-2-carboxylic acid
阿托伐他汀钙/雷米普利优化路线步数:6总收率:11.8g(Ramipril (Free))
5-[(2-Oxocyclopentyl)methyl]imidazolidine-2,4-dione→3-(2-Oxocyclopentyl)-L-alanine→(2S,3aS,6aS)-Octahydrocyclopenta[b]pyrrole-2-carboxylic acid→Benzyl (2S,3aS,6aS)-octahydrocyclopenta[b]pyrrole-2-carboxylate hydrochloride→Benzyl (2S,3aS,6aS)-octahydrocyclopenta[b]pyrrole-2-carboxylate→Ethyl (2S)-2-[[(2S)-1-chloro-1-oxopropan-2-yl]amino]-4-phenylbutanoate hydrochloride→N-[(S)-(+)-1-(Ethoxycarbonyl)-3-phenylpropyl]-L-alanine
阿托伐他汀钙/雷米普利优化路线步数:5总收率:19.67g(Ramipril-008)
2-Oxopropionic acid ethyl ester→Acetamide→Benzamide→Ethyl 2-acetamidoacrylate→Ethyl 2-(benzoylamino)acrylate→1-Morpholinocyclopentene→1-(1-Cyclopentenyl)pyrrolidine→Cyclopentanone→Ethyl N-acetyl-3-(2-oxocyclopentyl)alaninate→Ethyl N-benzoyl-3-(2-oxocyclopentyl)alaninate→Benzyl (2S,3aS,6aS)-octahydrocyclopenta[b]pyrrole-2-carboxylate hydrochloride

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