- 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
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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.
- Huang, Yande,Yu, Jaehoon,Bentrude, Wesley G.
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- DIAZEPINONE DERIVATIVES AND THEIR USE IN THE TREATMENT OF HEPATITIS B INFECTIONS
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Provided herein are compounds of formula (I) and (V) useful for the treatment of HBV infection in a subject in need thereof, pharmaceutical compositions thereof, and methods of inhibiting, suppressing, or preventing HBV infection in the subject.
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Page/Page column 340
(2018/02/28)
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- TRICYCLIC COMPOUNDS FOR USE AS KINASE INHIBITORS
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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).
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- Cyclic Organophosphorus Compounds XVII. The Mass Spectra of Some 5,5-Dimethyl-perhydro-1,3,2-oxazaphosph(v)orines
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The electron impect mass spectra of six 5,5-dimethyl and eleven 3,5,5-trimethyl-perhydro-1,3,2-oxazaphosphorine 2-oxides and 2-sulphides are reported and compared with those of analogous 5,5-dimethyl-1,3,2-dioxaphosph(v) orinans.Compounds of the 3,5,5-tri
- Edmundson, R. S.
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p. 558 - 564
(2007/10/02)
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