Patent PL-172609-B1 (PL)
Title: Method of obtaining derivatives of indolopyrrolocarbasole
Inventor: KOJIRI KATSUHISA
IPC: C07D487/12
Filed: 1992-11-27
Abstract: 1. The method of producing new derivatives of indole-pyrrole-carbazole presented in the general formula 1 and their pharmaceutically acceptable salts formula 1 IMAGE> where R1> and R2> refer independently of each other to a hydrogen atom or a group with the formula -Y-R3>, where Y refers to a carbonyl group, while R3> refers to a hydrogen atom, while R1> and R2> do not refer simultaneously to a hydrogen atom; G refers to a pentose group or a hexose group; while X1> and X2> refer independently of each other to an atom of hydrogen or a halogen, an amino group, a mono-lower-alkyl-amino group, a di-lower-alkyl-amino group, a hydroxyl group, a lower alkoxyl group, an aralkyloxyl group, a carboxyl group, a lower alkoxycarbonyl group or lower alkyl group. Characterized in that: The compound presented in the formula 2 below, or its derivative, where the functional groups are protected formula 2 IMAGE> where X1>, X2> and G have the meaning indicated above, R13> and R23> refer to hydrogen, is subjected to formylation, the protecting group(s) is(are) removed and the obtained compound is transformed into a pharmaceutically-acceptable salt. 2. The method of producing new derivatives of indole-pyrrole-carbazole presented in the general formula 1 and their pharmaceutically acceptable salts where R1 and R2 refer independently of each other to a hydrogen atom or a lower alkyl group, which can contain 1 to 5 substituents, selected from the following set of groups: carboxyl, carbamyl, sulphonic, amino, cyanic, mono-lower-alkyl-amino, di-lower-alyl-amino, hydroxyl group and a halogen atom, while R1> and R2> do not refer simultaneously to a hydrogen atom; G refers to a pentose group or a hexose group; while X1> and X2> refer independently of each other to an atom of hydrogen or a halogen, an amino group, a mono-lower-alkyl-amino group, a di-lower-alkyl-amino group, a hydroxyl group, a lower alkoxyl group, an aralkyloxyl group, a carboxyl group, a lower alkoxycarbonyl group or lower alkyl group. Characterized in that: The compound presented in the formula 2 below, or its derivative, where the functional groups are protected where X1>, X2> and G have the meaning indicated above, R13> and R23> refer to hydrogen, is subjected to alkylation, the protecting group(s) is(are) removed and the obtained compound is transformed into a pharmaceutically-acceptable salt. 3. The method of producing new derivatives of indole-pyrrole-carbazole presented in the general formula 1 and their pharmaceutically acceptable salts where R1> and R2> refer independently of each other to a hydrogen atom or a lower alkene group, which can contain 1 to 5 substituents, selected from the following set of groups: carboxyl, carbamyl, sulphonic, amino, cyanic, mono-lower-alkyl-amino, di-lower-alyl-amino, hydroxyl group and a halogen atom, while R1> and R2> do not refer simultaneously to a hydrogen atom; G refers to a pentose group or a hexose group; while  X1> and X2> refer independently of each other to an atom of hydrogen or a halogen, an amino group, a mono-lower-alkyl-amino group, a di-lower-alkyl-amino group, a hydroxyl group, a lower alkoxyl group, an aralkyloxyl group, a carboxyl group, a lower alkoxycarbonyl group or lower alkyl group. Characterized in that: The compound presented in the formula 2 below, or its derivative, where the functional groups are protected where X1, X2 and G have the meaning indicated above, R13 and R23 refer to hydrogen, is subjected to alkenation, the protecting group(s) is(are) removed and the obtained compound is transformed into a pharmaceutically-acceptable salt.