WATER SOLUBLE CRYSTALLIN SALTS OF CERTAIN HARRINGTONINES UNAMBIGUOUSLY PROTONATED ON THEIR ALKALOID NITROGEN AND THEIR USE AS CHEMOTHERAPEUTIC DRUGS

摘要

The present invention concerns harringtonine salts at the solid state exhibiting a protonated nitrogen seen in solid state analysis and having formula (1), comprising solvate, made by reacting a cephalotaxine ester having formula (2), in which R1 is, but not limited to, alkyl, aryl, cycloalkyl, heteroalkyl, heteroaryl or heterocycloalkyl, and R2 is, independently, but not limited to H, alkyl, aryl, cycloalkyl, heteroalkyl, heteroaryl or heterocycloalkyl, with an acid having general formula AH in a crystallization solvent, wherein the said salt has a water or alkohol solubility ranged approximately from 5 mg/mL to approximately 100 mg/Ml. The invention also related to a process for preparing these salts and their use as chemotherapeutic drugs.