Basilea Pharmaceutica Ag

Xiaoping Wu

Marc Muller

Lin Xu

C1-C6Alkyloxy- or benzyloxy-carbonyl esters of -{3-[(E)-(1-phenyl or naphthyl C1-C4alkyl)-imino]-propyl}-amino)-acetic acid, which are intermediates for producing known bridged monobactam compounds useful in the treatment of bacterial infections.

Bridged monobactam intermediates

A process for manufacturing a compound of Formula (I) which has cis-conformation and wherein R1 represents a 1-phenyl-C-Calkyl or 1-naphthyl-C-Calkyl group, wherein the phenyl or naphthyl moiety of R1 is unsubstituted or substituted with one or more C-Calkoxy groups and the carbon atoms in 2-, 3-, and/or 4-position of the alkyl part of R1 are, independently of the phenyl or naphthyl moiety of R1 and independently of one another, unsubstituted or substituted with C-Calkoxy and/or silyloxy or, preferably, are unsubstituted or substituted with one C-Calkoxy group and/or silyloxy group per carbon atom, and R2 represents a C-Calkyl group or an unsubstituted or substituted benzyl group, in which process a compound of Formula (II) wherein R3 represents a C-Calkyl group or an unsubstituted or substituted benzyl group, and R1 and R2 have the same meaning as in formula (I); is treated with a base at a temperature of 0&#xb0; C. or less in a liquid aprotic solvent for a time period sufficient to obtain the compound of formula (I). 

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Haimen, China

Xiaoping Wu