申请人:Research Corporation
公开号:US04261884A1
公开(公告)日:1981-04-14
A preparation of azlactones represented by the formula ##STR1## wherein R is a substituted or unsubstituted alkyl, aryl or nitrogen containing heterocyclic group, and R.sup.1 is an N-blocked amino acid residue or peptide chain, and stereoisomers thereof, by oxidizing the corresponding saturated azlactone with a benzoquinone oxidizing agent in the presence of a base is disclosed. The unsaturated azlactones, some of which are novel, can be converted to dehydro peptides, which are useful as intermediates for preparing novel biologically active compounds, or themselves have biological activity.
本发明揭示了一种由公式##STR1##所代表的含有取代或未取代的烷基,芳基或含氮杂环基团的azlactones制备方法,其中R.sup.1是N-阻断的氨基酸残基或肽链,以及其立体异构体,通过在碱的存在下使用苯醌氧化剂氧化相应的饱和azlactone来实现。其中一些为新颖的不饱和azlactones,可以转化为脱氢肽,用作制备新颖生物活性化合物的中间体,或者本身具有生物活性。