申请人:——
公开号:US20030013892A1
公开(公告)日:2003-01-16
Methods for production of chirally pure &agr;-amino acids and N-sulfonyl &agr;-amino acids are described. An aldehyde and a cyanide salt are reacted with an &agr;-methylbenzylamine to afford product. The product reacts with a strong acid, neutralized, and extracted. The resulting product is hydrolyzed to provide a product which is dissolved in a strong acid to provide a salt of a chirally pure &agr;-amino acid, which is reacted to provide the chirally pure a-amino acid. Another method involves mixing ephedrine hemihydrate and an N-sulfonyl &agr;-ethylnorvaline in ethanol at a molar ratio of 1:1; heating the mixture to dissolve the solids; cooling to allow formation of a precipitate; washing with an organic solvent to give diastereomeric salt; recrystallizing the salt; dissolving the recrystallized salt in an organic solvent and strong aqueous acid, separating the layers; washing the organic extract; drying and concentrating to provide chirally pure N-sulfonyl a-amino acid.
本文介绍了制备手性纯&agr;-氨基酸和N-磺酰基&agr;-氨基酸的方法。将醛和氰盐与&agr;-甲基苄胺反应,得到产物。产物与强酸反应,中和并提取。所得产物水解后,在强酸中溶解,得到手性纯&agr;-氨基酸的盐,反应得到手性纯a-氨基酸。另一种方法是将麻黄碱半水合物和N-磺酰基&agr;-乙基异戊氨酸以1:1的摩尔比例混合于乙醇中;加热混合物以溶解固体;冷却使其沉淀;用有机溶剂洗涤以得到对映异构体盐;重结晶盐;将重结晶盐在有机溶剂和强酸中溶解,分离层;洗涤有机提取物;干燥浓缩得到手性纯N-磺酰基&agr;-氨基酸。