학술논문
Harringtonines salts in the crystalline state and their use for the purification of the corresponding drug substance
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Patent
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Abstract
The present disclosure concerns harringtonines salts at the crystalline state exhibiting a protonated nitrogen seen in solid state analysis and having general formula 1, [chemical expression included] comprising solvates, made by reacting a cephalotaxine ester alkaloid base having formula 2, [chemical expression included] 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 non-aqueous crystallization solvent, wherein the said salt has a large water solubility. The disclosure is also related to a process for preparing and purifying these salts and their use as chemotherapeutic drugs.