775304-99-9Relevant academic research and scientific papers
Double cyclization of bis(α-hetarylmethyl)amino esters to optically active bridged N-heterocycles of HIV-inhibiting activity
Faltz, Heike,Bender, Christoph,Woehrl, Birgitta M.,Vogel-Bachmayr, Karin,Huebscher, Ullrich,Ramadan, Kristijan,Liebscher, Juergen
, p. 3484 - 3496 (2004)
Anellated 1-azabicyclo[3.3.1]nonanes 6 were synthesized by several routes starting from natural α-amino esters 2 and ohaloaryl- or o-bromohetarylmethyl bromides 1. N-Alkylation of the starting amino esters to 5 and 3 was followed by halogen/lithium exchange and double cyclization. The cyclization products 6 exhibit interesting inhibition of RNase H and DNA-polymerase activity of reverse transcriptase (RT) of HIV-1 at concentrations where human cellular DNA polymerases are not affected. Wiley-VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2004.
