| 摘要 |
(Poly)thia-alkynoic acid derivatives (I) are new. (Poly)thia-alkynoic acid derivatives of formula (I), and their optical and geometric isomers and salts, are new. Y = S, SO, SO2, CH2, CC or CH=CH; R1 = 1-18C alkyl (optionally substituted by one or more halo), 2-18C alkenyl or 2-18C alkynyl, all optionally interrupted by one or more of O, S and N; provided that (i) if Y = CH2, then R1 has 1-12 (preferably 6-12) atoms, (ii) if Y = CC, then R1 has 1-10 (preferably 6-10) atoms and (iii) if Y is other than CH2 and R1 is an unsaturated or heteroatom-containing group, then the unsaturation and/or heteroatom in R1 is not in the alpha -position relative to Y R2 = 1H-tetrazol-5-yl, CN, 4,5-dihydrooxazol-2-yl, CH2OR3 or COR4; R3 = H, 1-6C alkyl, 1-6C monohydroxyalkyl, 2-6C polyhydroxyalkyl, 3-6C cycloaliphatic group or tetrahydropyranyl; R4 = H, 1-6C alkyl, NR'R'' or OR5; R5 = H, 1-18C alkyl, 1-6C monohydroxyalkyl, 2-6C polyhydroxyalkyl (containing 2-5 OH), aryl or aralkyl (optionally substituted by one or more of 1-18C alkyl, COR''' and/or OR'''); R', R'' = H, 1-6C alkyl, 3-4C alkenyl, 3-6C cycloaliphatic group, aryl or aralkyl (both optionally substituted), aminoacid residue or aminosugar residue; or NR'R'' = heterocycle; R''' = H or 1-18C alkyl. |
