| 摘要 |
1320256 Azetidinones and cephalosporins ELI LILLY & CO 9 Sept 1971 [10 Sept 1970] 42179/71 Headings C2A and C2C Novel, therapeutic compounds (I) and (II) where A is phthalimido or RCONH-, R is H, ethoxycarbonyl, or C 1-8 alkyl, C 3-8 cycloalkyl or C 2-8 alkenyl optionally substituted with OH, SH, C 1-3 -alkoxy or -alkylthio or CN, or is a group of Formula (III), (IV) or (V) where Q is H, OH, SH, Cl, Br, C 1-3 -alkyl, -alkoxy or -alkylthio, NO 2 or CN, X is O, S or a direct bond, Y is OH, SH or NH 2 , m is 0, 1 or 2, n is 1 or 2, R<SP>1</SP> is -CH 2 OZ, -CH 2 O.CO.Z, -CONHZ or -CO 2 R<SP>11</SP> where R<SP>11</SP> is C 1-4 alkyl, C 4-6 tert-alkyl, C 5-8 tertalkenyl or -alkynyl, benzyl, methoxybenzyl, nitrobenzyl, benzhydryl, phthalimidomethyl, succinimidomethyl, phenacyl or trichloroethyl, Z is H, C 1-8 alkyl, C 3-8 cycloalkyl, or C 2-8 alkanyl, optionally substituted with OH, SH, C 1-3 -alkoxy or -alkylthio or CN or Z is phenyl or phenyl-C 1-3 -alkyl optionally substituted with OH, SH, Cl, Br, C 1-3 -alkyl, -alkoxy or -alkylthio, NO 2 or CN and W is Me, Et, Pr or Ph, are made by treating (VI) with triphenyl phosphine or trialkyl phosphite in the presence of acetic, propionic, butyric or benzoic anhydride (I is obtained; it is converted to the isomer II by treatment with base). Cephalosporins (VII) are obtained by oxidizing (I) or (II); (VII) can be dehydrated to give the corresponding unsaturated compound. |
