Preparation of Optically Pure Beta-Amino Acids Having Affinity for the Alpha-Delta Protein
申请人:Herrinton Paul Matthew
公开号:US20080194841A1
公开(公告)日:2008-08-14
Disclosed are materials and methods for preparing optically active β-amino acids, which bind to the alpha-2-delta subunit of a calcium channel and are useful for treating pain, fibromyalgia, and a variety of psychiatric and sleep disorders. The method includes reacting a chiral allyl amine with a 2-alkynoate in the presence of a Lewis acid and a base to give a chiral tertiary enamine, which after reaction with ammonia, is hydrogenated to give optically active β-amino acids.
本发明涉及制备光学活性β-氨基酸的材料和方法,该氨基酸与钙通道的α-2-δ亚单位结合,并且用于治疗疼痛、纤维肌痛和各种精神和睡眠障碍。该方法包括在路易斯酸和碱的存在下,将手性丙烯基胺与2-炔酸酯反应,得到手性三级恩酰胺,然后与氨反应后,经过氢化作用得到光学活性β-氨基酸。