STEREOSELECTIVE PROCESS AND CRYSTALLINE FORM OF CAMPTOTHECIN

摘要

PROBLEM TO BE SOLVED: To provide a stereoselective process for leading to each of single E, Z isomers, more particularly the E isomer of a camptothecin derivative bearing alkyloxime O-substituted at position 7.

SOLUTION: A stereoselective process for preparing 7-[(E)-t-butyloxyiminomethyl]-camptothecin is disclosed. With the addition of further dissolution and precipitation steps carried out in appropriate different solvent mixtures, four new crystalline forms of gimatecan can be obtained by using the same stereoselective process.

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