METHOD FOR MANUFACTURING OF IMIDOAMINE BIS-ADDUCT OF MALEOPIMARIC ACID METIL ESTER WITH DIMETHYL-HEXAAZAPERHYDROPYRENE SPACER AND ITS USE AS A DRUG WITH CYTOTOXIC ACTIVITY Russian patent published in 2023 - IPC C07D487/22 A61K31/395 A61K31/403 A61K31/53 A61P35/00 

FIELD: synthesis of biologically active compounds.

SUBSTANCE: method for the production of 2,4,6-trimethyl-5-{2-[2,4,6-trimethyl-5-{2-[2,4,6-trimethyl-1,3,5-dithiazinan-5-il]-ethyl}-1,3,5-thiadiazinan-3-il]-ethyl}-1,3,5-dithiazinan. The invention relates to the field of synthesis of biologically active compounds, specifically to method for the production of bis-adduct of maleopimaric acid methyl ester (MPAME) imidoamine with dimethyl-hexaazaperhydropyrene spacer of formula (1). The essence of the method is the interaction of 2,6-dimethyl-1,4,5,8-tetraazadecaline with N,N,N',N'-tetramethylmethanediamine and MPAME imidoamine in the presence of catalyst NiCl₂ ⋅ 6H₂O at a molecular ratio of 2,6-dimethyl-1,4,5,8-tetraazadecalin : N,N,N',N'- tetramethylmethanediamine : MPAME imidoamine : NiCl₂ ⋅ 6 H₂O = 1 : 4 : 2 : (0.03-0.07) in CH₃OH-H₂O medium at ~20° C and atmospheric pressure for 2.5–3.5 h. The yield of bis-adduct of MPAME imidoamine with dimethyl-hexaazaperhydropyrene spacer (1) is 14-24%.

EFFECT: technical result of the invention is production of bis-adduct of maleopimaric acid methyl ester imidoamine with dimethyl-hexaazaperhydropyrene spacer of formula (1), which has cytotoxic activity against human cancer cells (HTC-116, SH-SY5Y, MCF-7, A549, Jurkat, THP-1).

1 cl, 2 tbl, 5 ex