16047-86-2Relevant articles and documents
Study of the Conformational Equilibria of 2-Z-3-Methyl-1,3,2-oxazaphosphorinanes. Steric and Stereoelectronic Influences on the Orientation of the Me2N Substituent on Three-Coordinate Phosphorus
Huang, Yande,Yu, Jaehoon,Bentrude, Wesley G.
, p. 4767 - 4773 (1995)
The conformations of a series of 1,3,2-oxazaphosphorinanes containing tree-coordinate phosphorus, 1-9, have been determined by the use of 1H, 31P, and 13C NMR spectroscopy.The rings were substituted at ring nitrogen, N(3), with a methyl group to compare its effect on conformational energies with those of 1,3,2-oxazaphosphorinanes reported earlier that featured a larger substituent at N(3), Ph or i-Pr.Quite expectedly, like those rings previously studied with Ph or i-Pr at N(3), a MeO or (CF3)2CHO substituent at phosphorus has a strong preference to be axial on a chair-form ring, 1-4, cis-7, and cis-8, or pseudoaxial on a ring in a twist/boat conformation, trans-7.However, when Me2N is attached to phosphorus, the newly studied N(3)Me rings display a chair-chair conformational equilibrium, 10 ->///- 11 is opposite to that found for four-coordinate phosphorus containing 1,3,2-oxazaphosphorinanes in which Me2NP(ax)/N(3)Ph repulsions that destabilize 10 appear to be dominant.
TRICYCLIC COMPOUNDS FOR USE AS KINASE INHIBITORS
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Page/Page column 67, (2013/03/26)
There is provided compounds of formula (I), wherein R1, R2, X, R3 and R4 have meanings given in the description (and which compounds are optionally substituted as indicated in the description), and pharmaceutically-acceptable esters, amides, solvates or salts thereof, which compounds are useful in the treatment of diseases in which inhibition of a protein or lipid kinase (e.g. a PIM family kinase, such as PIM-1, PIM-2 and/or PIM-3) is desired and/or required, and particularly in the treatment of cancer or a proliferative disease. There is also provided combinations comprising the compounds of formula (I).
