Phenyl-carboxy-alkyl-di- or tetra:hydro-furanone derivs.

摘要

EP--99692 A Di- or tetrahydrofuranone derivs. of formula (I) and their salts are new: (where A is lower alkylene R1 is COOH, opt. protected OH, lower alkoxycarbonyl, lower alkoxycarbonylamino or lower alkanoyloxy; R2 is H, halogen or lower haloalkyl; R3 is H or halogen; R4 is H, OH, COOH, lower alkoxy, lower alkanoyloxy or lower alkoxycarbonyloxy and R5 is H or halogen, or R4+R5 is =CH2, or R3+R4 or R3+R5 is a bond). - Also claimed is a biologically pure culture of the microorganism Chaetomella raphigera FERM BP-293 capable of producing FR-51785 substance (disclosed as being 3-(4-hydroxy-5-oxo -3-phenyl-2,5-dihydro -2-furyl)propionic acid). - (I) are aldose reductase inhibitors and may be used for treating diabetic cataract and neuropathy. (0/0) EPAB- EP--99692 B Compounds of the general formula (I), wherein A is a C1-C5 alkylene group; R1 is a car-oxyl, hydroxyl, protected hydroxyl, (C1-C5 alkoxy)carbonyl, (C1-C5 alkoxy)-carbonylamino or C1-C5 alkanoyloxy group; R2 is a hydrogen or halogen atom or a halo(C1-C5)alkyl group; R1 is a hydrogen or halogen atom; R4 is a hydrogen atom or a hydroxyl, carboxyl, C1-C5 alkoxy, C1-C5 alkanoyloxy or (C1-C5 alkoxy)-carbonyloxy group and R5 is a hydrogen or halogen atom or R4 and R5 together form a =CH2 group; the heavy solid line means a single or double bond and n is 0 or 1, with the proviso that when the heavy solid line means a single bond, n is 1 and when the heavy solid line means a double bond, n is 0; and the pharmaceutically acceptable salts thereof. - (50pp) USAB- US4797417 A Furanone derivs. of formula (I) and salts are new. In (I), A is 1-4C alkylene; R1 is COO, OH, BzO, 1-5C alkoxycarbonyl; R2 is H, halo, halo (1-5C) alkyl; R3 is H, OH, COO, 1-5C-alkoxy or -alkoxycarbonyl. Esp. cpd. is ethyl 3-(4-methoxy-5 -oxo-3-phenyl-2,5 -dihydro-2-furyl) propionate. (I) may be prepd. e.g. by reacting (II) with (III).