NOVEL COMPOUNDS OF REVERES TURN MIMETICS, THE PROCESS OF PREPARATION AND THE USE THEREOF

摘要

PURPOSE: A pharmaceutical composition containing reverse-turn mimetic with pyrazino-triazinone as a basic structure is provided to effectively suppress proliferation of acute myeloid leukemia cells. CONSTITUTION: A novel compound of reverse-turn mimetics is denoted by chemical formula I. A pharmaceutical composition contains the compound of chemical formula I and pharmaceutically acceptable excipient. A method for treating acute myelocytic leukemia(AML) comprises a step of administering effective amount of the pharmaceutical composition to a patient with AML. A method for preparing the compound of chemical formula I comprises: a step of introducing an acyl group to indole-7-carbaldehyde by Friedel-Crafts acylation to prepare 3-acyl-indole-7-carbaldehyde; a step of introducing alkyl groups and amino acetal groups to 3-acyl-indole-7-carbaldehyde to prepare a 1-alkyl-3-acyl-indole derivative; a step of performing amidation to prepare reaction intermediates; a step of cyclizing to prepare a cyclic intermediate; and a step of phosphating the cyclic intermediate.