74115-13-2Relevant articles and documents
Synthesis of novel 7-substituted pyrido[2′,3′:4,5]furo[3,2-d] pyrimidin-4-amines and their N-aryl analogues and evaluation of their inhibitory activity against Ser/Thr kinases
Deau, Emmanuel,Loidreau, Yvonnick,Marchand, Pascal,Nourrisson, Marie-Renee,Loaec, Nadege,Meijer, Laurent,Levacher, Vincent,Besson, Thierry
, p. 6784 - 6788 (2014/01/06)
The efficient synthesis of 7-substituted pyrido[2′,3′:4,5] furo[3,2-d]pyrimidin-4-amines and their N-aryl analogues is described. 3,5-Dibromopyridine was converted into 3-amino-6-bromofuro[3,2-b]pyridine-2- carbonitrile intermediate which was formylated with DMFDMA. Functionalization at position 7 of the tricyclic scaffold was accomplished, before or after cyclisation step, by palladium-catalyzed Suzuki-Miyaura cross-coupling while the pyrimidin-4-amines and N-aryl counterparts were synthesized by microwave-assisted formamide degradation and Dimroth rearrangement, respectively. The final products were evaluated for their potent inhibition of a series of five Ser/Thr kinases (CDK5/p25, CK1δ/ε, CLK1, DYRK1A, GSK3α/β). Compound 35 showed the best inhibitory activity with an IC50 value of 49 nM and proved to be specific to CLK1 among the panel of tested kinases.
A convenient route to functionalized 3-amino-6-bromofuro[3,2-b]pyridine-2-carboxamides
Bretéché, Anne,Marchand, Pascal,Nourrisson, Marie-Renée,De Nanteuil, Guillaume,Duflos, Muriel
experimental part, p. 4490 - 4494 (2010/07/06)
An efficient synthesis of 3-amino-6-bromofuro[3,2-b]pyridine-2-carboxamides is described via the formation of 3-amino-6-bromofuro[3,2-b]pyridine-2-carbonitrile. Functionalization of the amino group at position 3 of the heterocycle will be discussed.
ANDROGEN MODULATORS
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Page/Page column 28, (2009/07/17)
The present invention is directed to a new class of benzonitriles and to their use as androgen receptor modulators. Other aspects of the invention are directed to the use of these compounds to decrease excess sebum secretions and to stimulate hair growth.