A Convenient and General Method for the Preparation of tert-Butoxycarbonylaminoalkanenitriles and Their Conversion to Mono-tert-butoxycarbonylalkanediamines
A new method is described for the synthesis of tert-butoxycarbonylaminoalkanenitriles 3 by dehydration of the corresponding carboxamides 2 (prepared in two steps from aminoalkanoic acids) in the presence of trifluoroacetic anhydride and triethylamine.N-Boc-aminoalkanenitriles 3 are easily converted to mono-N-Boc-alkanediamines 4 under mild conditions avoiding the cleavage of the N-protective group.The monoprotected alkanediamines 4 are useful tools in affinity chromatography.
Six tetrazole analogues of GABA-mimetic compounds were synthesized. In vitro only two compounds, analogues of GABA and isoguvacine, showed a weak affinity for GABA-A and GABA-B receptors. In vivo compounds were inactive in a psychopharmacological screening in mice. The results were interpreted in terms of intercharge distance, electronic delocalisation and ability of membrane crossing.
Schlewer,Wermuth,Chambon
p. 181 - 186
(2007/10/02)
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