9,10-α,α-OH-taxane analogs and methods for production thereof
AssigneeTapestry Pharmaceuticals, Inc.
InventorsJan Zygmunt, James Ferrara, James D. McChesney
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AssigneeTapestry Pharmaceuticals, Inc.
InventorsJan Zygmunt, James Ferrara, James D. McChesney
Estimating the term…
The present invention relates to taxane analogs for the treatment of cancer having the general formula: wherein R1 and R2 are each selected from H, an alkyl group, an olefinic group, an aromatic group, an O-alkyl group, an O-olefinic group, or an O-aromatic group; R3 is hydroxyl or OP1; R4 and R5 are each hydroxyl or R7COO; R6 is hydroxyl, OP2, R7COO, or an ether functionality; R7 is an alkyl group, an olefinic group, or an aromatic group; P1 and P2 are each hydroxyl protecting groups; R8 and R9 are each selected from H, alkyl group, olefinic or aromatic group. The present invention is also directed to production methods and intermediates useful in the formation of these new taxane analogs. The methods may begin with a starting compound, such as paclitaxel or docetaxel, which is converted into a taxane analog through various intermediate compounds.
A method for producing taxane analogs and compounds comprising treating a compound represented by either Formula G′ or Formula M′ with a compound of generalized formula R8R9C(OCH3)2 and an acid selected from the group consisting of camphor sulfonic acid (CSA), p-toluene sulfonic acid (PTSA), hydrochloric acid (HCl) and acetic acid (AcOH):
Dependencies are inferred from the claim text.