METHOD FOR SYNTHESIS DI- AND TRIAMINOCHLORINES Russian patent published in 2007 - IPC C07D487/22 A61K31/409 A61P35/00 

FIELD: organic chemistry.

SUBSTANCE: invention relates to a method for synthesis of e₆ chlorine derivatives with two or three amino-groups. The proposed method provides to synthesize chlorines comprising 2 and 3 amino-groups without using activating agent and with high yields that are similar or exceed yields of analogous compounds prepared by using activating agents. In using the proposed methods di- and triaminochlorines can be synthesized selectively from methylpheophorbid (a) directly without isolation of intermediate compounds. Method for synthesis of aminochlorines involves interaction of ester groups of chlorine e₆ with ethylenediamine and isolation of the end product wherein pure ethylenediamine is used, chlorine e₆ 13-N-(2-aminoethylamide)-15,17-dimethyl ester is synthesized in situ from methylpheophorbid (a) and 50-200-fold mole excess of ethylenediamine in chloroform medium at room temperature 15-25°C for 1.5-2.5 h followed by evaporation of chloroform in rotor evaporator under reduced pressure 20-300 mm mercury column and at bath temperature 50°C, not above. Before isolation the reaction mixture is kept in dark at room temperature and after keeping the mixture for 20 h e₆ chlorine diamine is isolated as the end product that comprises two amino-groups, and after keeping the mixture for 70 h e₆ chlorine triamide is isolated comprising tree amino-groups. The proposed method of synthesis chlorines can be used in synthesis of antitumor and antiviral preparations in medicinal aims.

EFFECT: improved method of synthesis.

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