申请人:Sumitomo Chemical Company, Limited
公开号:US04059603A1
公开(公告)日:1977-11-22
The amidation and esterification of carboxylic acids with amines and hydroxyl group-containing compounds, respectively, are effected without incurring the drawbacks of reaction equilibrium by the reaction of the reactants, one of which has been activated in the reactive group by contact with a phosphonium salt obtained by reacting a phosphorous ester or phosphorous monoester salt with an organic base such as pyridine and an oxidizing agent such as halogens and mono or divalent mercury halide or acetate. The amidation can be applied to the preparation of peptides by the reaction of amino acids and/or peptides in which one of the reactive groups have been protected.
通过羧酸与胺或含有羟基的化合物进行酰胺化和酯化反应,其中一个反应物已被磷盐活化,可以避免反应平衡的缺点。磷盐是通过将磷酸酯或磷单酯盐与有机碱(如吡啶)和氧化剂(如卤素和一价或二价汞卤化物或醋酸盐)反应而得到的。酰胺化可以应用于肽的制备,通过对氨基酸和/或肽进行反应,其中一个反应基团已被保护。