申请人:Sumitomo Chemical Company, Limited
公开号:US03974219A1
公开(公告)日:1976-08-10
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 meercury 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.
羧酸与胺和含有羟基化合物的酰胺化和酯化分别进行,通过与反应物之一发生反应而不产生反应平衡的缺点,其中其中一个已经通过与有机碱(如吡啶)和氧化剂(如卤素和单价或二价汞卤化物或乙酸盐)反应得到的磷酯或磷单酯盐制得的磷盐接触而在反应基团中被激活。酰胺化可以应用于通过氨基酸和/或肽的反应制备肽,其中其中一个反应基团已被保护。