Convenient and simplified approaches to N-monoprotected triaminopropane derivatives: Key intermediates for bifunctional chelating agent synthesis

[摘要]：High yields of selectively N-protected-1,2,3-triaminopropanes (1,3 or 1,2 functionalized diamines) were obtained in 6 or 4 steps from diamino alcohols or aminodiols, respectively. These two multi-step procedures involve protection of (he amino group, substitution of the hydroxy group by an azido group and selective reduction. The conditions for the first procedure allow the preparation of various N-2-monoprotected-1,2,3-triaminopropanes 6a, 6b, but the second one is more convenient for obtaining N-1-Boc-1,2,3-triaminopropane 6'. These two simplified procedures, which provide functionalized 1,2 or 1,3 diamines easily and with good overall yields, could be useful for the synthesis of bifunctional chelating agents.

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