METHOD FOR DEACETYLATION OF α-AMINOACETALS Russian patent published in 2013 - IPC C07C269/04 C07C271/16 C07C271/18 C07C271/22 

FIELD: chemistry.

SUBSTANCE: invention relates to a method of producing N-substituted α-aminoaldehydes in a racemic or optically active form, involving the following steps: (a) protecting the amine functional group of the corresponding α-aminoacetals by introducing an arylalkyloxycarbonyl group of general formula , wherein R is hydrogen, a phenyl group or a linear or branched C₁-C₆ alkyl group, Ar is a phenyl group, a naphthyl group or an anthryl group, optionally substituted with one or more halogen atoms, one or more phenyl groups, linear or branched C₁-C₆ alkyl groups, linear or branched C₁-C₆ alkoxy groups, nitro, cyano or methyl thionyl groups; (b) deacetylation of the acetal functional group of said N-protected α-aminoacetals with formic acid. The invention also relates to a compound of formula , (R)-(II) or (S)-(II), where R₁ and R₂, identical or different, denote a linear or branched C₁-C₁₂ alkyl group; R₃ is a cycloalkylalkyl group in which the cycloalkyl group is a C₃-C₁₀ cycloalkyl group and the linear or branched alkyl group is a C₁-C₁₂ alkyl group; P is a benzyloxycarbonyl group and the symbol (*) denotes that the carbon atom is an asymmetric atom.

EFFECT: obtaining N-protected α-aminoaldehydes while preserving protection of the amine functional group which is suitable for industrial scale.

8 cl, 1 tbl, 11 ex