19690-37-0Relevant articles and documents
Synthesis and biological evaluation of a triazole-based library of pyrido[2,3-d]pyrimidines as FGFR3 tyrosine kinase inhibitors
Le Corre, Laurent,Girard, Anne-Lise,Aubertin, Johannes,Radvanyi, Franois,Benoist-Lasselin, Catherine,Jonquoy, Aurelie,Mugniery, Emilie,Legeai-Mallet, Laurence,Busca, Patricia,Le Merrer, Yves
scheme or table, p. 2164 - 2173 (2010/07/04)
A library of pyrido[2,3-d]pyrimidines was designed as inhibitors of FGFR3 tyrosine kinase allowing possible interactions with an unexploited region of the ATP binding-site. This library was built-up with an efficient step of click-chemistry giving easy access to triazole-based compounds bearing a large panel of substituents. Among the 27 analogues synthesized, more than half exhibited 55-89% inhibition of in vitro FGFR3 kinase activity at 2 μM and one (19g) was able to inhibit auto-phosphorylation of mutant FGFR3-K650M in transfected HEK cells.
NUCLEOPHILIC CHARACTERISTICS OF NUCLEOFUGIC ANIONS IN THE CLEAVAGE OF EPOXIDES BY PROTIC ACIDS AND NITRONIUM FLUOROBORATE
Zefirov, N. S.,Kirin, V. N.,Yur'eva, N. M.,Zhdankin, V. V.,Kozmin, A. S.
, p. 1264 - 1279 (2007/10/02)
The cleavage of ethylene, propylene, and cyclohexene oxides by protic acids RCOOH (R= CH3, CF3) in the presence of sources of nucleophilic anions (the lithium or tetrabutylammonium salts of perchloric or substituted sulfonic acids) leads to the formation not only of 2-hydroxyalkyl carboxylates but also of significant amounts of 2-hydroxyalkyl perchlorates and sulfonates.In the reactions of the same oxides with nitronium fluoroborate and the above-mentioned salts in methylene chloride 2-perchloryl- and 2-sulfonyloxyalkyl nitrates are formed with high yields; these are the products from opening of the epoxide ring and subsequent combination of the perchlorate and substituted sulfonate ions.The investigated processes extend the range of reactions involving the concurrent combination of nucleofugic anions and can be used as a method for the production of β-hydroxy- and β-nitroxyalkyl perchlorates and sulfonates.
