Patent ID: 6828445
Filing Date: 2004-12-07
Classification: A61P,C07D,Y02P

Abstract:
A process for the preparation of 14&bgr;-hydroxy-1,14-carbonate-deacetylbaccatin III, which comprises the following steps:a. protection of the hydroxyls at the 7- and 10-positions of 10-deacetylbaccatin III: wherein R and R1 are selected from hydrogen, C1-C10 alkyl or aryl, C1-C10 alkyl- or aryl-carbonyl, trichloroacetyl, C1-C4 trialkylsilyl; preferably, when R and R1 are the same, they are trichloroacetyl, whereas when they are different, preferably R is trichloroacetyl and R1 is acetyl, or R is triethyl or trimethylsilyl and R1 is acetyl; b. two-step oxidation to give the derivative oxidised to carbonyl at the 13-position and hydroxylated at the 14-position: c. carbonation of the vicinal hydroxyls at the 1- and 14-positions to give the 1,14-carbonate derivative: d. reduction of the carbonyl at the 13-position: e. removal of the protective groups at the 7- and 10-positions: