| 摘要 |
<p>NEW MATERIAL:A propargylglycine derivative of formula I: [X is (CH3)2, formula IV (R3 is H, or acetoxy group); R1 is H, lower alkylcarbonyl, 4-lower alkyl-2,3-dioxo-1-piperazynocarbonyl group, etc,; R2 is H or alkyl group], and its non-toxic salt. EXAMPLE:6-(alpha-amino-alpha-propargylacetamido) penicillanic acid. USE:Antibacterials. PROCESS:A compound of formula II: (R4 is R1, amino-protecting group) or its reactive derivation is reacted with a compound of formula III: (R5 is H or ester residue) or its salt in a solvent, e.g. THF or acetone, preferably at -20 deg.C to room temperature, and, if necessary, the amino-protecting group is removed to give the compound of formula I. When an acid is formed by the reaction, a base, e.g. alkali carbonate or picoline is added.</p> |
