FIELD: chemistry.
SUBSTANCE: method includes reacting a compound of formula (II) with a compound of formula (III) in alkaline conditions and in the presence of a sulphite. In formulae I, II and III (*) denotes a chiral centre; R1 is a straight or branched alkyl containing 1-4 carbon atoms; R2 is hydrogen, a straight or branched alkyl containing 1-4 carbon atoms; R3 is a straight or branched alkyl containing 1-6 carbon atoms, an alkoxy, a cycloalkoxy, a phenyl or a substituted phenyl, a heterocyclyl; and R4 is an alkyl, a haloalkyl, an aryl, or a substituted aryl, where the substitute includes oxo, halogen, hydroxy, cyano, nitro, amino, alkylamino, dialkylamino, alkyl, alkoxy, haloalkyl, aryl, heterocyclyl, -NRaRb, -NRaC(=O)Rb, NRaC(=O)NRaRb, -NRaC(=O)ORb, -NRaS(=O)2Rb, -ORa, -C(=O)Ra-C(=O)ORa, -C(=O)NRaRb, -OCH2C(=O)NRaRb, -OC(=O)NRaRb, -SH, -SRa, -SORa, -S(=O)2NRaRb, -S(=O)2Ra, -SRaC(=O)NRaRb, -OS(=O)2Ra and -S(=O)2ORa, where Ra and Rb are identical or different and are independently hydrogen, alkyl, haloalkyl, alkoxy or aryl; the compound of formula (I) and compound of formula (II) are present in an R or S configuration of a racemic mixture. The molar ratio of the sulphite to the compound of formula (II) is (0.8-2.5):1 and the molar ratio of the compound of formula (III) to the compound of formula (II) is (1.1-5.0):1.
EFFECT: method is suitable for extensive industrial production and enables to obtain a product with high output.
18 cl, 3 tbl, 20 ex
Authors
Dates
2015-07-27—Published
2012-06-21—Filed