摘要:
A process for the production of a 3-vinylcephalosporin compound of formula I wherein R1 and R2 may be the same or different and denote hydrogen or an organic radical, which comprises subjecting a 3-iodomethyl-cephalosporin to a Wittig reaction in the presence of a weak base.
摘要:
1. A process for preparing a 3-alkenylcephem compound or 3-norcephem compound of the formula (3) characterized in that an alkenyl halide of the formula (2), a nickel catalyst, a metal up to −0.3 (V/SCE) in standard oxidation reduction potential and a compound of a metal having a higher standard oxidation reduction potential than the metal are caused to act on a 3-cephem compound of the formula (1) in a solvent wherein R1 is a hydrogen atom or the like, R2 is a hydrogen atom or the like, R3 is a hydrogen atom or carboxylic acid protective group, and X is a halogen atom or the like, R4—Y (2) wherein R4 is 1-alkenyl having or not having a substituent, and Y is a halogen atom wherein R1, R2 and R3 are as defined above, and R5 is a hydrogen atom or 1-alkenyl having or not having a substituent.
摘要:
A process for preparing 3-alkenylcephem compounds characterized in that 3-alkenylcephem compound of the formula (3) is prepared in a single step by simultaneously conducting reactions of a 3-chloromethylcephem compound of the formula (1) with iodization reagent, alkali metal hydroxide or carbonate, arylphosphine and an aldehyde of the formula (2) R4—CHO (2) wherein R1, R2, R3 and R4 are as defined in the specification.
摘要:
A process for the production of a 3-vinylcephalosporin compound of formula I wherein R1 and R2 denote hydrogen or an organic group by a Wittig reaction reacting first a compound of formula II with a compound of formula P(R4)3 or P(OR4)3 to produce a compound of formula III and secondly reacting the compound of formula III with a weak base of formula or of formula R10—COO−W+ wherein R5 is hydrogen, alkly or aryl and R6 and R7 are each an activated group of formula —COOR8, —CN, —SO2R8, —COR8 or —CON(R8)2; or R5 and R8 are each aryl and R7 is an activated group of formula —COOR8, —CN, —SO2R8, —COR8 or —CON(R8)2, W+ is an alkali metal cation and R10 is alkyl or aryl to produce a compound of formula IV and finally reacting a compound of formula IV with a compound of formula V to produce a compound of formula I.
摘要:
The present invention relates to novel processes for the preparation of 3-methylenecephams. More specifically, the present invention relates to the intramolecular cyclization of penicillin sulfoxide derived monocyclic azetidinone derivatives with organometallic catalysts of the formula III. MEx(H2O)y (III) wherein: M is Sc, Y, La, Ce, Pr, Nd, Sm, Eu, Gd, Tb, Dy, Ho, Er, Tm, Yb, Lu, Zr, Hf, Th, Nb, Ta, U, Bi, or In; E is O[SO2(C1-C6 polyfluoroalkyl)], N[SO2(C1-C6 polyfluoroalkyl)]2, or C[SO2(C1-C6 polyfluoroalkyl)]3; x is 3; y is 0, 1, 2, 3, 4, 5, 6, 7, 8, or 9.
摘要:
Derivatives of 7-alkylidene cephalosporanic acid sulfone and the pharmaceutically active salts thereof are found to be potent inhibitors of &bgr;-lactamase enzymes.
摘要:
A process for the purification of cefixime via a novel tert-octylamine salt of a cefixime intermediate of formula V which may be crystalline and which may be produced in a one-pot reaction from 7-amino-3-vinyl-ceph-3-em-4-carboxylic acid.