The process of su00ecntese racu00eamica drug (+) - 4 - (3 - ciclopentilu00f3xi - 4 - metu00f3xifenil) - pirrolidin - 2 - one (rolipram) and two new analogues of baclofen

摘要

"The process of su00ecntese racu00eamica drug ( sym ) - 4 - (3 - ciclopentilu00f3xi - 4 - metu00f3xifenil) - pirrolidin - 2 - one (rolipram) and two new analogues of baclofen.New process of obtaining and / or synthesis of ( sym ) - 4 - (3 - ciclopentilu00f3xi - 4 - metu00f3xifenil) - pirrolidin - 2 - one and two new analogues of baclofen, commonly used in the pharmaceutical industry.Especially in the manufacture of anti-inflammatory drugs.The process consists in the synthesis of 2 - ciclopentilu00f3xi - 4 - nitroanisol (3); starting from (3) we obtain the synthesis of hydrochloride of 3 - ciclopentilu00f3xi - 4 - metu00f3xianilina (4); starting from (4) we obtain theSynthesis of tetrafluoroborate ciclopentilu00f3xi - 4 - 3 - metu00f3xi - benzenediazonium (5); on the basis of (5) are obtained in the synthesis of 1 - (T - butu00f3xicarbonil) - 4 - (3 - ciclopentilu00f3xi - 4 - metu00f3xifenil) - pirrolidin2 - ol (6); partindThe (6) are obtained in the synthesis of 1 - (T - butu00f3xicarbonil) - 4 - (3 - ciclopentilu00f3xi - 4 - metu00f3xifenil) - pirrolidin - 2 - one (7); starting from (7) are synthesis of 4 - (3ciclopentilu00f3xi - 4 - metu00f3xifenil) - pirrolidin - 2 - one (1),That is the end product of more interest and principal in the process; starting from (1) we obtain the synthesis of hydrochloride of 4-amino-3 - (3 - hydroxy - 4 - metu00f3xifenil) - butyric acid (2a), which is another product finAl in the process; also from (7) are obtained in the synthesis of acid 4 - t - butu00f3xicarbonilamino - 3 - (3 - ciclopentilu00f3xi - 4 - metu00f3xifenil) - butyric acid (8),And finally, on the basis of (8) are obtained in the synthesis of hydrochloride of 4-amino-3 - (3 - ciclopentilu00f3xi - 4 - metu00f3xifenil) - butyric acid (2b), which is the other end product of this process.