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Sucinimidyl esters are used, inter alia, as activated acyl derivatives, in particular when other acylating agents, such as acid chlorides or anhydrides, cannot be employed on account of the lability of startingmaterials or final products. This applies particularly in the field of peptide chemistry. For coupling a covalent peptide bond, an activated carboxyl component is necessary. The previously most frequently used method for carboxyl activation is basedon the formation of succinimidyl esters by reaction of the corresponding carboxylic acid with carbodiimides, such as, for example, N,N'-dicyclohexylcarbodiimide (DCC) and N-hydroxysuccinimide. The disadvantage in this process lies, on the one hand, inthe coupling reagent DCC on account of its allergenicity and of the high price, and, on the other hand, in the by-product N,N'-dicyclohexylurea obtained here, which firstly contaminates the succinimidyl ester and secondly has to be disposed of. For these reasons, it was attempted to replace the system DCC/N-hydroxysuccinimide. Possible alternatives are systems of the type halophosphoric acid ester/N-hydroxysuccinimide/base.[/size]¾ÍÊÇÕâÀï×îºóÒ»¸öbase£¬ÊÇɶÒâ˼£¿ÎÒ²»ÊÇѧÉúÎïµÄ ΪÁËÓÐÓï¾³£¬°ÑÈ«²¿Ò»¶Î¶¼Ð´ÁË£¬ÍøÉÏËѵÄÒ»¶ÎרÀûÎÄÏ×£¬ÁôÏÂÀ´ÎÒÒ²ºÃÕҵõ½![]() http://www.patentgenius.com/patent/5929251.html |
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