METHOD FOR OBTAINING (3BR*,7AR*,10BR*,14AR*-CIS-14C,14D)-2,9-BIS(PYRIDIN-3-YLMETHYL)OCTADECAHYDRO-1H,8H-2,3A,7B,9,10A, 14B-HEXAAZADIBENZO[FG,OP]TETRACENE AND ITS USE AS AN AGENT WITH CYTOTOXIC ACTIVITY Russian patent published in 2023 - IPC C07D487/22 A61K31/53 A61P35/00 

FIELD: biologically active compounds.

SUBSTANCE: method for obtaining 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-yl] ethyl}-1,3,5-dithiazinan. The invention relates to the field of biologically active compounds, namely (3b R *, 7a R *, 10b R *, 14a R * - cis -14c, 14d) -2,9-bis (pyridin-3-ylmethyl) octadecahydro-1 H,8H-2,3a,7b,9,10a,14b-hexaazadibenzo[ fg,op ]tetracene of formula (1), which has cytotoxic activity against cell lines of human hepatocellular carcinoma (HepG2), colon adenocarcinoma (HTC-116 ), human monocytic leukemia (THP-1), breast carcinoma (MCF-7), lung adenocarcinoma (A549), T-cell leukemia (Jurkat), and human neuroblastoma (SH-SY5Y). The invention also relates to a process for the preparation of tetracene of formula (1). The method consists in the interaction of trans - 1,6,7,12-tetraazaperhydrotetracene with N,N,N',N' -tetramethylmethanediamine and 3-methylaminopyridine in the presence of a NiCl₂6H₂O catalyst at a molar ratio of trans-1,6,7,12-tetraazaperhydrotetracene: N,N,N',N' -tetramethylmethanediamine : 3-methylaminopyridine: NiCl₂·6H₂O = 1:4:2:(0,03-0,07). The reaction is carried out in a CH₃OH medium at room temperature (~20°C) and atmospheric pressure for 2.5–3.5 h.

EFFECT: obtaining tetracene of formula (1) with a yield of 32–39%.

3 cl, 2 tbl, 5 ex