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