ADD Organic Operations (Department 04KA, Building AP-8B) Diagnostics Division, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, Illinois 60064-6016, United States.
J Org Chem. 2011 Nov 4;76(21):9169-74. doi: 10.1021/jo201686e. Epub 2011 Oct 3.
A method for the in situ formation of N-trifluoroacetoxy succinimide (TFA-NHS) and its application in the formation of succinimidyl esters is presented. The developed method provides N-trifluoroacetyl and N-maleoyl amino acid succinimidyl esters from a variety of amino acids using a one-pot, high-yielding protocol. Investigations into the formation of an N-maleoyl amino acid succinimidyl ester supported the proposal of a revised reaction mechanism, and contributed to the optimization of the reaction conditions.
本文介绍了一种原位生成 N-三氟乙酰亚胺基琥珀酰亚胺（TFA-NHS）的方法及其在琥珀酰亚胺酯形成中的应用。该方法采用一锅法高产率的方法，从多种氨基酸中得到 N-三氟乙酰和 N-马来酰基氨基酸琥珀酰亚胺酯。对 N-马来酰基氨基酸琥珀酰亚胺酯形成的研究支持了修订的反应机制的提出，并有助于优化反应条件。
