P-toluenosulfonate salt of N-Methyl-N-(3,5-dimathoxy-2,4,6-triazinyl-1-)-morpholine and related compounds for use as condensing reagent in peptide synthesis

摘要

The invention refers to new quarternary N-(3,5-disubstituted-1,3,5-triazinyl-1)-ammonium salts of sulfonic acids, with formula 1, where R1 and R2 denote in total or independently a halogen atom, an alkyl group, a substituted alkyl group, an alkoxy group, a substituted alkoxy group, a cycloalcoxy group, a substituted cycloalkoxy group, an aryl group, a substituted aryl group, an aryloxy group, a substituted aryloxy group, a heterocyclic group or a substituted heterocyclic group, preferably the methoxy group, where R3, R4, R5 denote independently each other an alkyl group, a substituted alkyl group, a cycloalkyl group, a substituted cycloalkyl group, an aryl group, a substituted aryl group, a heterocyclic or a substituted heterocyclic group, or form a heterocyclic ring with nitrogen atom, whereas O-SO2R6 denotes a sulfate anion, hydrosulfonate anion, arylsulfonate anion, preferable benzenosulfonate anion, p-toluenosulfonate anion, p-bromobenzenosulfonate anion, p-chlorobenzenosulfonate anion, alkylosulfonate anion, preferable methanosulfonate and trifluoromethanesulfonate anions or amidosulfonate anion. <??>The new compounds are designed for application as condensing reagents in syntheses of amides, esters, carboxylic acid hydroxides, and particularly in synthesis of peptides and their esters. <IMAGE>