专利号:WO-2005049567-A1 优先权日:2003-11-24 标题:A novel synthesis of 2-azabicyclic-3-carboxylic acids, useful as important drug intermediates 发明人:BABU POTLURI RAMESH; HARIHARAKRISHNAN VENKATA SUBRA; SRIHARI TADIMALLA VENKATA; PRASAD KODALI HARI; RAMESH BETINI; MALLAPARAJU GOTTIMUKKALA VENKA 权利人:BABU POTLURI RAMESH; HARIHARAKRISHNAN VENKATA SUBRA; SRIHARI TADIMALLA VENKATA; PRASAD KODALI HARI; RAMESH BETINI; MALLAPARAJU GOTTIMUKKALA VENKA 摘要:A novel process for the preparation of 2-azabicyclo-3-carboxylic acid hydrochloride of formula (I), by reacting the compound of formula (II) with an acylating agent in a non-polar solvent at 0-150 °C to give a compound of formula (III), which is reacted with an enamine of formula (IV) in a non-polar solvent in the presence of an organic base at 0 °C to 150 °C to yield a compound of formula (V), which is hydrolytically cyclised to give a compound of formula (VI) and further catalytically hydrogenated to give the compound of formula (I).
专利号:EP-1692106-A1 优先权日:2003-11-24 标 题:A novel synthesis of 2-azabicyclic-3-carboxylic acids, useful as important drug intermediates