Preparation of taxanes from 9-dihydro-13-acetylbaccatin III
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United States of America Patent
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Sep 11, 2012
Grant Date -
Mar 5, 2009
app pub date -
Mar 30, 2006
filing date -
Mar 31, 2005
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Abstract
The present invention relates to a new process for the preparation of 9-dihydrobaccatin III intermediates as useful precursors for the preparation of paclitaxel, 1, docetaxel, 2, and analogues thereof. More particularly, the process comprises the steps of (i) concomitantly deacetylating esters at the 10-position and 13-position of 9-dihydro-13-acetylbaccatin III to form 9-dihydro-10-deacetylbaccatin III; (ii) protecting a hydroxy group at the 7-position of 9-dihydro-10-deacetylbaccatin III; and (iii) acylating a hydroxy group at the 10-position to form a compound of formula II.
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