| 摘要 |
Azetidinones of formula (I) are new (R1 is opt. substd. amino, substd. OH, N3 or halo. R3 is H, hydroxymethyl, arylalkoxylminomethyl, aryl, aralkenyl, formyl, carboxy or a nucleophile residue. R3 is CHR4R5 or -CR5=CR6R7. R4 = aryl, aralkyl, arylthioalkyl or heterocyclyl, R5 = COOH or one of its derivs. R6 = alkyl, haloalkyl, heterocyclythioalkyl, or arylthio. R7 = H, haloalkyl or heterocyclylthioalkyl; provided that (A) when R1 = NH2 or acylamino derived from carboxylic or sulphonic acid, and R2 = H, then R3 is CHR4R5, CR5=CR6R7 or CR5=CHR8, with R4 = phenyl substd. by opt. N-substd. alkanesulphonamido or aroylalkoxy, naphthyl, aralkyl, arylthioalkyl or heterocyclyl. R6 = alkyl, haloalkyl or heterocyclyl thioalkyl. R7 = haloalkyl or heterocyclythioalkyl. R8 = arylthio. (B) when R1 is opt. substd. amino or N3, and R2 = aryl, halo or residue of an S-contg. nucleophile, then R6 = alkyl or heterocyclylic thioalkyl; R7 is heterocyclic thioalkyl; R8 is arylthio. Alkane, arene and heterocyclic gps. are opt. substd.). (I) are antibacterials useful for treating Gram positive and negative inections in animal including humans. The usual dose is 1-2g/day. A typical cpd., 0.2-(2-oxo-3-phthalimido-1-azetidinyl)-2-(2-thienyl)acetate, was prepd. from 2-phthalimidoacetyl chloride and 1,3,5-tris D-1-(2-thienyl)-1-methoxycarbonylmethyl perhydro-1,3,5- -triazine. |
