发明授权
US5006661A Selective stereospecific biologically active beta-lactams 失效
选择性立体定向生物活性β-内酰胺

Selective stereospecific biologically active beta-lactams
摘要:
The present invention relates to a method for producing novel 4-[1-oxoalkyl]-2,5-oxazolidinediones, (4-1 OOD), and their use in a stereoselective method of producing beta-lactam-containing compounds which include several biologically active compounds such as the well-known families of pencillin and cephalosporin antibiotics. The method of the present invention involves generally the reaction of the above-described 4-[1-oxoalkyl]-2,5-oxazolidinediones so produced with a thiol amine having a geometry amenable to forming the precursor of the desired beta-lactam-containing compound or, in one scheme, forming the beta-lactam-containing compound itelf directly. This is done either by direct reaction of the 4-1 ODD with a thiol amine (which by one pathway proceeds directly to the beta-lactam-containing compound) or by first converting the 4-1 OOD to its 2-[1-oxoalkyl]-2-amino acid form before its reaction with the thiol amine; and then forming the beta lactam by action of cyanogen). The beta-lactam-containing compounds can be further modified according to methods known in the art to produce specific derivatives as desired.
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