Taxol Derivatives With Antitumor Activity

A preparation method of the compound of the formula (I):

• at least one of R1 and R2 independently represents at least one of hydrogen, alkyl, halogen-substituted alkyl and a group composed of at least one of R1, R2, N and O selected from the groups consisting of:
• Z1 represents hydrogen, hydroxyl, halogen, or C1-C3 alkyl;
• Z2 represents hydrogen, hydroxyl, halogen, or C1-C3 alkyl;
• Z3 represents at least one of C1-C6 alkyl, C2-C6 alkenyl, C3-C6 cycloalkyl, monocyclic five-membered C6-C10 aryl, monocylcic six-membered C6-C10 aryl, and C6-C10, wherein one of said alkyl, alkenyl, alkynyl, cycloalkyl aryl and heterocyclic group is optionally substituted by at least one group from the group consisting of halogen, hydroxyl, carboxylic, C1-C3 alkyl, C1-C3 alkoxyl, phenyl, amino, C1-C3 alkylamino, C1-C3 alkoxyl carbonyl, C6-C10 aryloxy carbonyl, acyl, amido and acyloxy;
• and
• Z4 represents C1-C6 alkyl, C6-C10 aryl and C1-C6 alkoxy, wherein at least one of said alkyl, aryl and alkoxy is optionally substituted by at least one group selected from the group consisting of halogen, hydroxyl, carboxylic, C1-C3 alkyl, C1-C3 alkoxyl, phenyl, amino, C1-C3 alkylamino, C1-C3 alkoxyl carbonyl, C6-C10 aryloxy carbonyl, acyl, amido and acyloxy, said method comprising the steps of:

A compound of the salts of the formula (I):

• at least one of R1 and R2 independently represents at least one of hydrogen, alkyl, halogen-substituted alkyl and a group composed of at least one of R1, R2, N and O selected from the groups consisting of
• Z1 represents hydrogen, hydroxyl, halogen, or C1-C3 alkyl;
• Z2 represents hydrogen, hydroxyl, halogen, or C1-C3 alkyl;
• Z3 represents at least one of C1-C6 alkyl, C2-C6 alkenyl, C3-C6 cycloalkyl, monocyclic five-numbered C6-C10 aryl, monocyclic six-membered C6-C10 aryl, and C6-C10, wherein one of said alkyl, alkenyl, alkynyl, cycloalkyl aryl and heterocyclic group is optionally substituted by at least one group from the group consisting of halogen, hydroxyl, carboxylic, C1-C3 alkyl, C1-C3 alkoxyl, phenyl, amino, C1-C3 alkylamino, C1-C3 alkoxyl carbonyl, C6-C10 aryloxy carbonyl, acyl, amido and acyloxy;
• and
• Z4 represents C1-C6 alkyl, C6-C10 aryl and C1-C6 alkoxy, wherein at least one of said alkyl, aryl and alkoxy is optionally substituted by at least one group selected from the group consisting of halogen, hydroxyl, carboxylic, C1-C3 alkyl, C1-C3 alkoxyl, phenyl, amino, C1-C3 alkylamino, C1-C3 alkoxyl carbonyl, C6-C10 aryloxy carbonyl, acyl, amido and acyloxy.