Enantioselective synthesis of both enantiomers of 2-amino-6-phosphonohexanoic acid [(R)- and (S)-AP6], a potent and specific agonist of AMPA receptor subtype
作者:Oscar García-Barradas、Eusebio Juaristi
DOI:10.1016/s0957-4166(97)00162-6
日期:1997.5
of both enantiomers of 2-amino-6-phosphonohexanoic acid [(R)- and (S)-AP6] is described. The highly diastereoselective alkylation of imidazolidinones 4 and hydrolysis of the alkylated products [(2R,5R,1′S)-6 and (2S,5S,1′S)-6] proceeds under relatively mild conditions to give the physiologically important, enantiopure aminophosphonic acids (R)-AP6 and (S)-AP6.
描述了2-氨基-6-膦酸己酸[(R)-和(S)-AP6]的两种对映体的制备。咪唑烷酮4的高度非对映选择性烷基化和烷基化产物[(2R,5R,1'S)-6和(2S,5S,1'S)-6 ]的水解在相对温和的条件下进行,从而提供了重要的生理上对映纯的物质氨基膦酸(R)-AP6和(S)-AP6。