1039021-95-8Relevant articles and documents
C-H FLUORINATION OF HETEROCYCLES WITH SILVER (II) FLUORIDE
-
Paragraph 00168, (2015/02/19)
The present invention provides compositions and methods for the selective C-H fluorination of nitrogen-containing heteroarenes with AgF2, which has previously been considered too reactive for practical, selective C-H fluorination. Fluorinated heteroarenes are prevalent in numerous pharmaceuticals, agrochemicals and materials. However, the reactions used to introduce fluorine into these molecules require pre-functionalized substrates or the use of F2 gas. The present invention provides a mild and general method for the C-H fluorination of nitrogen-containing heteroarene compounds to 2-fluoro-heteroarenes with commercially available AgF2. In various embodiments, these reactions occur at ambient temperature within one hour and occur with exclusive selectivity for fluorination at the 2-position. Exemplary reaction conditions are effective for fluorinating diazine heteroarenes to form a single fluorinated isomer.
Discovery of piperidin-4-yl-aminopyrimidines as HIV-1 reverse transcriptase inhibitors. N-Benzyl derivatives with broad potency against resistant mutant viruses
Kertesz, Denis J.,Brotherton-Pleiss, Christine,Yang, Minmin,Wang, Zhanguo,Lin, Xianfeng,Qiu, Zongxing,Hirschfeld, Donald R.,Gleason, Shelley,Mirzadegan, Taraneh,Dunten, Pete W.,Harris, Seth F.,Villasenor, Armando G.,Hang, Julie Qi,Heilek, Gabrielle M.,Klumpp, Klaus
scheme or table, p. 4215 - 4218 (2010/08/22)
An analysis of the binding motifs of known HIV-1 non-nucleoside reverse transcriptase inhibitors has led to discovery of novel piperidine-linked aminopyrimidine derivatives with broad activity against wild-type as well as drug-resistant mutant viruses. Notably, the series retains potency against the K103 N/Y181C and Y188L mutants, among others. Thus, the N-benzyl compound 5k has a particularly attractive profile. Synthesis and SAR are presented and discussed, as well as crystal structures relating to the binding motifs.
Non-nucleoside reverse transcriptase inhibitors
-
Page/Page column 39; 43, (2008/12/06)
The present invention provides for compounds useful for treating an HIV infection, or preventing an HIV infection, or treating AIDS or ARC. The compounds of the invention are of formula I wherein R1, R2, R3, R4, R5a, R5b, R6a, R6b and X are as herein defined. Also disclosed in the present invention are methods of treating an HIV infection with compounds defined herein and pharmaceutical compositions containing said compounds.