A method for the preparation of the taxol analog 10 - deacetyltaxol a, b and c

摘要

pThe present invention relates to an improved process for the production of important taxol analogues 10-deacetyl taxol A,B and C of the formula (2) R=C6H5(10 deacetyl taxol A) =CH3C=CHCH3 (10-deacetyl taxol B) =C5H11 (10-deacetyl taxol C) where R represent C6H5 (10-deacetyl taxol A) or, CH3C=CHCH3 (10-deacetyl taxol B) or, C5H11 (10-deacetyl taxol C) which comprises (a) dissolving the taxol analogues 7-xylosyl-10-deacetyl taxol A,B,C of the formula (1) R=C6H5 (10 deacetyl taxol A) =CH3C=CHCH3 (10-deacetyl taxol B) =C5H11 (10-deacetyl taxol C) where R represents C6H5 (taxol analogue A or xyloside A), or CH3C=CHCH3 (taxol analogue B or xyloside B) or C5H11 (taxol analogue C or xyloside C) in a polar solvent (b) reacting the resultant solution with periodate for 20-40 hours at 20-40 DEG C. to cleave the diol system of the xyloside into dialdehyde, (c) treating the generated dialdehyde in a mixture of polar solvent-organic acid mixture with salts of amines at 0-40 DEG C. for 12-18 hours and (d) isolating the 10-deacetyl taxol A,B,C by chromatography./p [US6028206A]