摘要 |
<p>Cpds of formula (I): (where R is alkylene or CR5R6; R5 is H, Me or MeS; R6 is alkyl, alkylthio, aryl, arylthio, aralkyl, aryloxy or a heterocyclic gp or R5+R6 forms an opt. substd ring e.g. cycloalkyl or a heterocyclic gp; X is H, acetoxy 1-3C alkoxy or SY, where Y is alkyl alkenyl or a nucleophilic gp) or their non-toxic salts, are prepd by acylating the corresp. 4-ACA with a cpd (II): (where R1 and R2 are 1-3C alkyl or NR1R2 is piperidino or morpholino, R3 is 1-3C alkyl and R4 is H or 1-3C alkyl or R3 + R4 forms a cyclopentyl or cyclohexyl ring) or a functional acid deriv (pref. mixed anhydride) to give a cpd (III): and hydrolysing this. Cpds (I) have antibacterial activity.</p> |