Non-ring hydroxy substituted taxanes and methods for synthesizing the same

摘要

The invention relates to (among other things) non-ring hydroxy substituted taxanes and methods for synthesizing the same. The invention further relates to conjugating the non-ring hydroxyl substituted taxanes to a water-soluble, non-peptidic polymer.

主权项

1. A method comprising esterifying a baccatin III compound of Formula III, which compound is encompassed by the formula:wherein:
R1 is selected from the group consisting of H, a hydroxy protecting group, a C1-6 organic radical; R2 is selected from the group consisting of H, a hydroxy protecting group, a C1-6 organic radical; and R3 is H or a hydroxy protecting group, with an ester linkage-providing compound of Formula II, which compound is encompassed by the formula:wherein:
R4 is C6H5— or  and each of D7, D8, D9, D10, D11, D12, D13, D14 and D15 is independently selected from the group consisting of H, dueterium; L1 is alkylene having 1-10 carbon atoms; PG is an amino protecting group; andeither: (i) R5 is H and R6 is —OH; or (ii) R5 and R6 represent a single covalent bond between the nitrogen to which R5 is attached and the carbonyl carbon to which R6 is attached.