| 摘要 |
PROBLEM TO BE SOLVED: To obtain the subject new derivative having a medicinal property more improved than rapamycin, a marked stability and in vivo utility, and easily capable of formulating a Galenical preparation and useful as an immunosuppressin agent, or the like. SOLUTION: This compound is expressed by the formula [X is (H, H) or O; Y is (H, OH) or O; R<1> and R<2> are each H, an allyl, or the like R<4> is methyl, or forms a 2-6C alkylene together with R<1> ; both of R<1> and R<2> are not H and excepting 40-0-(2-hydroxy)ethylrapamycin], i.e., 40-O-(2-hydroxy) ethoxycarbonylmethyl-rapamycin, 40-O-[(3S)-2,2-dimethyldioxolan-3-y1]methyl- rapamycin or 40-0-[2-(4',5'-dicarboethoxy-1',2',3'-triazol-1'-y1)-ethyl]-rapamycin is exemplified. The compound of the formula is obtained by, e.g. reacting rapamycin with diphenyldiselenide and tributylphosphine. |
