To obtain a new derivative composed of a specific 4'-O- trifluoromethanesulfonyl-daunorubicin derivative as an intermediate or the like for production of 4'-epi-daunorubicin, an antitumor antibiotic useful as a medicine against tumors and the like.
The intermediates are a new 4'-O-trifluoromethanesulfonyl- daunorubicin derivative shown by formula I (R1 is H, and R2 is a protective group for an amino group, where R1 and R2 work together as a protective group for an amino group), and a 4'-epi-4'-O-acyl-daunorubicin derivative shown by formula II (R3 is H, or a (substituted) lower alkyl, (substituted) aryl or aralkyl), each useful as an intermediate or the like for production of 4'-epi- daunorubicin, an antitumor antibiotic useful as a medicine against tumors and the like. Each of these compounds is produced by reacting daunorubicin with a protected amino acid, shown by formula III, with trifluoromethanesulfonic acid anhydride or a carboxylic acid in the presence of 4-dimethylaminopyridine.
| JP2014526480 | Crystallization of Idarubicin hydrochloride |
| WO/1996/002659 | IT-62-B SUBSTANCE AND MEDICINAL COMPOSITION CONTAINING THE SAME |
| WO/2014/060408 | ANTHRACYLINE DERIVATIVES FOR TREATING TUMOR DISEASES |
MATSUMOTO NAOKI
NAGAI HAZUKI
ISSHIKI KUNIO
YOSHIOKA TAKEO
Next Patent: NEW POLYHYDRO DERIVATIVE OF TYROSINE AND PRODUCTION THEREOF