PHYSIOLOGICALLY ACTIVE BIS-DIALKYLAMIDES OF PHOSPHORYL-SUBSTITUTED 1,4-DICARBOXYLIC ACIDS AND METHOD FOR PRODUCING SAME
申请人:Federalnoe Gosudarstvennoe Bydzhetnoe Uchrezhdenie
Nauki Institut Fiziologicheski Aktivnikh Veschestv
Rossiiskoi Akademii Nauk (IFAV RAN)
公开号:EP2660245A1
公开(公告)日:2013-11-06
To produce physiologically active bis-dialkylamides of phosphorylated 1,4-dicarboxylic acids of formula (I)
wherein each R can be straight or branched alkyl, unsubstituted or substituted phenyl, wherein substituents of the phenyl group can be from 1 to 5 halogen atoms, from 1 to 5 lower alkyl groups, from 1 to 5 lower alkoxy groups, from 1 to 5 dialkylamino groups; R' can be straight or branched alkyl; Y is a direct bond or a methylene group, a mixture of the corresponding phosphorylated 1,4-dicarboxylic acids is heated with hexaalkyl triamidophosphites of general formula (R'2N)3P in an organic solvent within a temperature range from 20 to 80°C until the reaction is complete followed by separation and purification. The compounds of general formula (I) thereby produced possess neuroprotective properties and can be used in medicine.
生产具有生理活性的式 (I) 磷酸化 1,4-二羧酸双二烷基酰胺
其中每个 R 可以是直链或支链烷基、未取代或取代的苯基,苯基的取代基可以是 1 至 5 个卤素原子、1 至 5 个低级烷基、1 至 5 个低级烷氧基、1 至 5 个二烷基氨基;R'可以是直链或支链烷基;将相应的磷酸化 1,4-二羧酸混合物与通式为(R'2N)3P 的六烷基三脒基膦酸在有机溶剂中加热,温度范围为 20 至 80°C,直至反应完全,然后进行分离和纯化。由此制得的通式(I)化合物具有神经保护特性,可用于医药。