摘要 |
<p>A novel process for producing N<4>-acyl-5'-deoxy-5-fluorocytidine derivatives using the novel 5'-deoxy-5-fluoro-N<4>,2'-O,3'-O-triacylcytidine derivatives are provided. 5-Deoxy-1,2,3-tri-O-acyl- beta -D-ribofuranoside is reacted with 5-fluorocytosine to produce 5'-deoxy-2',3'-di-O-acyl-5-fluorocytidine, followed by acylation. The acyl radicals of the obtained 5'-deoxy-5-fluoro-N<4>,2'-O,3'-O-triacylcytidine derivatives are selectively de-O-acylated to obtain N<4>-acyl-5'-deoxy-5-fluorocytidine derivatives. From fluorocytosine, N<4>-acyl-5'-deoxy-5-fluorocytidine derivatives can be obtained through very few steps in high yield.</p> |
申请人 |
F. HOFFMANN-LA ROCHE AG, BASEL, CH;FUJI KAGAKU KOGYO K.K., TOYAMA, JP |
发明人 |
KAMIYA, TAKASHI, OSAKA-HU, JP;ISHIDUKA, MAKOTO, TOYAMA-SHI, TOYAMA-KEN, JP;NAKAJIMA, HIROSHI, TOYAMA-SHI, TOYAMA-KEN, JP |