Catalyst and method for amide formation

The invention is a catalyst, the use of the catalyst and a method of using the catalyst in the formation of a compound with an amide bond. The catalyst is an HOBT derivative having the following formula (1): where R1 is a group bearing a positive charge at pH 5-7; where Y is a bond or a substituted...

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1. Verfasser: SCOTT WILLIAM LEONARD
Format: Patent
Sprache:eng
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Zusammenfassung:The invention is a catalyst, the use of the catalyst and a method of using the catalyst in the formation of a compound with an amide bond. The catalyst is an HOBT derivative having the following formula (1): where R1 is a group bearing a positive charge at pH 5-7; where Y is a bond or a substituted or unsubstituted alkylene chain containing 1-10 carbon atoms and 0-2 heteroatoms selected from the group consisting of N, S and O; and where X is a linker group selected from -CO- or -SO2-. In the method, an amine, a carboxylic acid, an amide coupling agent and a catalyst of formula (1) are reacted for a time sufficient to produce an amide bond between the amine and the carboxylic acid. Thereafter, the compound containing the amide bond is isolated.