Methods for preparing 1-deoxy paclitaxels

摘要

Preparation (A) of 1-deoxy-7,9-acetonide paclitaxel analogues (I) comprises: (a) deactylating 1-deoxybaccatin VI to form a 7,9,10-trisdeacetyl derivative (II); (b) modifying (II) to form a 7,9-acetonide derivative (III); (c) protecting a hydroxy substituent at C-10 of 1-deoxybaccatin VI with a hydroxy protecting group; (d) forming a C-13 deacetyl derivative of the product of (c); (e) esterifying the C-13 deacetyl derivative of (d) with a 3-hydroxy-4-phenyl beta -lactam (IV) in which the 3-hydroxy group is protected with a protecting group; and (f) deprotecting both the C-2' position resulting from (e) and the C-10 position.