PROCESS FOR PREPARING C-SUBSTITUTED DIETHYLENE TRIAMINES

摘要

A process for preparing C-substituted diethylene triamines having general formula (I) is characterized in that a nitrogen-protected aminoethyl alcohol having general formula (II) is reacted with methane sulphonic acid chloride, tosyl chloride or trifluoroacetic acid anhydride in an organic solvent, with addition of a base, to give the corresponding mesylate, tosylate or triflate, is then filtered and the filtrate is reacted with an ethylene diamine having general formula (III) to give the desired nitrogenprotected, carbon-substituted triamine having general formula (I), in which R1 stands for a -(CH2)m-(C6H4)q-(O)k-(CH2)n- (C6H4)l-(O)r-R group or for a -(CH2)m-(C6H10)q-(O)k-(CH2)n- (C6H10)l-(O)r-R group; R2 and R3 each stand for a hydrogen atom or form together a -(CH2)p-alkylene bridge; and R4 stands for an amino protecting group, preferably for a benzyloxycarbonyl group.