| 摘要 |
FIELD: chemistry.SUBSTANCE: invention refers to a new method for producing antifolate agents having a glutamic acid fragment in their structure, or their salts of the general formula(I). The method involves carrying out a reaction of a compound of formula(I) and an acid or a base in a solution. The compounds of formula (II) are produced by carrying out a reaction of N-substituted glutamic acids or their salts with chloroacetonitrile. In formula (I), M means a monovalent or bivalent cation specified in a group consisting of Na, K, 1/2Caor 1/2Mg; R means a group. In the above group, Rrepresents a carbonyl group; Rand Rare identical or different and specified in linear or branched, saturated or unsaturated C-C-heteroalkyl groups, which can be optionally substituted by amino groups; aromatic or aliphatic C-C-hydrocarbon rings, which can be optionally substituted by one or more substitutes specified in a group consisting of alkyl, alkenyl, alkynyl, carboxy, hydroxy, amine, nitro, thiol, sulphoxy, sulphonic groups; aromatic or aliphatic C-C-heterocycles, which can be optionally substituted by one or more substitutes, specified in a group consisting of alkyl, alkenyl, alkynyl,carboxy, hydroxy, amine, nitro, thiol, sulphoxy, sulphonic groups; together Rand Rcan both form a phenyl or thiophen ring, which can be substituted by an alkyl group or an alkyl group containing heteroatoms; and the alkyl groups can be additionally substituted by bicyclic or heterocyclic ring systems containing such structures, as purines or pyrimidines. In formula (II), R has the value as specified in formula (I).EFFECT: method enables producing the high-yield antifolate agents of formula (I) with high analytical and optical purity.14 cl, 4 ex |
