| 摘要 |
<p>The invention relates to a process for the preparation of antibacterial panem compound of the formula I <IMAGE> wherein R is <IMAGE> wherein either R10 is trifluoro lower alkyl and R11 is trifluoro lower alkyl or dihydroxy lower alkyl; or R10 is hydrogen and R11 is substituted thiazolyl, imidazolyl, substituted alkyl or <IMAGE> and <IMAGE> wherein R13, R14 and R15 are hydrogen or alkyl or R15 and R16 taken together with nitrogen form a 3-6 membered heterocyclic ring, or R is (a) an optionally substituted heterocyclic group or (b) R is -CH2-S-Het, wherein Het is a heterocyclic group or (c) R is -(CH2)n-Ar, wherein n=0 or 1 and Ar is a substituted phenyl group or (d) R is -CH2-(r)n-Hat, wherein n=0 or 1 and Hat is 3 or a heterocyclic group of 5 ring atoms or (e) R is monoalkyl or dihydroxy (lower) alkyl or (f) R is carboxylic acid, carboxylate, amino acid, nitrile, ketone, amide or ether and (g) R is amine, imine or cyclic urea, X is hydrogen, a pharmaceutically acceptable salt forming group, a pharmaceutically acceptable ester group or a carboxy protecting group, or a tautomer thereof, when R is hydrogen.</p> |
