THYMOL DERIVATIVE HAVING CARCINOSTATIC ACTIVITY AND CARCINOSTATIC AGENT INCLUDING THE SAME

摘要

PROBLEM TO BE SOLVED: To obtain the subject new compound exhibiting excellent carcinostatic activity by reacting m-cresol with dihydroxyacetophenone as starting materials. SOLUTION: This thymol derivative is expressed by formula I (R1 is acetyl or hydroxy which may be protected with isobutyryl, methyl or the like; R2 is H, acetyl, isobutyryl, palmitoyl or the like; R3 and R4 are each epoxy, diol or an olefin; R5 is hydroxy which may be protected with acetyl or isobutyryl, methyl or H) or its pharmaceutically permissible salt or ester, e.g. 10- isobutyryloxy-8,9-epoxythymol isobutyrate. The compound of formula I is obtained by obtaining an intermediate of formula II by using m-cresol as a starting material, introducing a hydroxy group to allyl site of a double bond by using selenium dioxide as a catalyst, further bonding various acids to newly generated hydroxy group to obtain a compound of formula III, then subjecting to epoxidation reaction.