Cephalosporin analogs

Details Cephalosporin analogs Cephalosporin analogs

C - Chemistry, Metallurgy

07

D

260/271

C07D 471/04 (2006.01) C07D 463/00 (2006.01) C07F 9/568 (2006.01)

Patent

CA 1133903

A B S T R A C T The present invention relates to a process of producing novel cephalosporin analogs represented by the general formula [I-2] Image [I-2] (wherein R1 represents a hydrogen atom, a halo group, a hydroxy group, a lower alkoxy group, a lower alkylthio group, an arylthio group, an aralkylthio group, a lower alkylsulfinyl group, a lower alkylsulfonyl group, an arylsulfonyl group or an aralkylsulfonyl group, R2 may be the same as R1 mentioned above or represents an acyloxy group, a lower alkyl group, a lower alkyl group substituted with halogens, an azido group, a nitrile group or an amino group represented by the general formula NR9R10 wherein R9 and R10 may be the same or different and represent a hydrogen atom, a lower alkyl, aryl or aralkyl group, and R3 represents a hydrogen atom or a substituted or unsubstituted alkyl, aryl, aralkyl or silyl group), which comprises converting X1 group of the compound represented by the general formula [I-1] Image [I-1] (wherein X1 represents an azido group or a phthalimido group and R1, R2 and R3 have the same significance as defined above) by reduction or deprotection to an amino group, and if necessary, when R3 is an alkyl group, an aryl group, an aralkyl group or a silyl group, con- verting the COOR3 group to COOH group in a conventional manner. The compounds [I-2] are useful intermediates in the preparation of analogs of Cephalothin.

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