Intermediates for the production of picropodophyllin and...

C - Chemistry – Metallurgy – 07 – C

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260/352.1, 260/6

C07C 43/225 (2006.01) C07D 317/48 (2006.01)

Patent

CA 1182827

ABSTRACT OF THE DISCLOSURE The present invention provides compounds useful as intermediates in the preparation of antineoplastic agents, having the structure: Image VI wherein R1 represents alkoxy or aralkoxy, R2 represents hydrogen, alkoxy, aralkoxy, alkyl, aralkyl, or R1 and R2 taken together represent the group -O-CH2-O-, R3 repre- sents hydrogen, alkyl, aralkyl, acyl or a protecting group, Y represents Cl, Br, I or a leaving group; and X represents Cl, Br or I. The present invention also provides a process for preparation of compounds VI in a single step wherein X and Y are the same and represent Cl, Br, or I, and R3 is as previously defined except that in this instance, it does not represent a protecting group.

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