|[Molecules: 18] [Related articles/posters: 024 018 052 001 063 ]|
A new route to aminodiazines is reported, the ortho-directed lithiation of diazines is used, followed by reaction with tosylazide as an electrophile. The reduction of the azido or tetrazolo compounds obtained was achieved and led to the expected amines. This methodology has allowed to synthesis of new aminodiazines and an improvement in the yield of various aminodiazines previously described.
As an application to the new route to aminodiazines, we report the synthesis of an aza analogue 2 of the Nevirapine 1 , a highly selective non-competitive inhibitor of HIV-1 reverse transcriptase.
As an application to the new route to aminodiazines, we report here the synthesis of an aza analogue of the Nevirapine 1. Nevirapine is a highly selective, non-competitive inhibitor of HIV-1 reverse transcriptase which is currently undergoing phase II clinical evaluation for the treatment of HIV-infected individuals. The synthesic sequence of the aza analogue 2 is outlined in Scheme 5.