| 摘要 |
<p>PURPOSE:To obtain in an industrially advantageous way the subject compound having antineoplastic activity, useful as a medicine, etc., by protecting the hy droxyl group in the saccharide segment of an etoposide with halogenoacetyl group followed by introducing phosphate group into the 4'-site and then eliminat ing the halogenoacetyl group. CONSTITUTION:4'-o-benzyloxycarbonyl-4'-dimethyl-epipodophyllotoxin is made to react under cooling with beta-D-2,3-di-o-dichloroacetyl-4,6-o-ethylideneglucopyranose in the presence of boron trifluoride-diethyl ether followed by addition of palladium black and then introduction of hydrogen into the system to carry out debenzyloxycarbonylation. Thence, the resulting product is made to react with phosphorus oxychloride followed by hydrolysis to form a compound of formula I [R and R' are each of formula COCHmX3-m. (X is halogen; m is 0-2)], which is, in turn, treated with e.g. triethylamine to eliminate the protecting group for the hydroxyl group in the saccharide segment, thus obtaining the objective etoposide phosphoric ester of formula II.</p> |
