| 摘要 |
NEW MATERIAL:To compound expressed by formula I (R<1> is 3-7C unsaturated alkyl, etc.; R<2> is H or halogen; R<3> is H or lower alkyl; X is carboxyl), salt thereof and ester and amide thereof. EXAMPLE:[2-(1-Cyclohexenyl)-4-oxo-4H-[1]-benzopyran-8-yl]acetic acid. USE:An antitumor agent capable of raising activity of natural killer cell when administered to a bioorganism and extremely suitable in administration with interleukin-2. PREPARATION:A compound expressed by formula II is reacted with an ester expressed by the formula R<4>COOEt (R<4> is hydrogenated R<1>) in the presence of a base to give a compound expressed by formula IV, which is then subjected to ring closure using a catalyst such as trifluoroacetic acid. Then the resultant compound expressed by formula V is brominated to afford a compound expressed by formula VI (R<4>' is R<4> brominated at alpha-position), which is further cyanidated to give a nitrile expressed by formula VII. Then the nitrile expressed by formula VII is subjected to solvolysis to provided the compound expressed by formula I. |
