- IMIDAZO[1,2-B]PYRIDAZINE IL-17A INHIBITORS
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The invention provides certain difluorocyclohexyl-imidazopyridazinyl-imidazolidinone compounds of formula II as IL-17A inhibitors, pharmaceutical compositions thereof, and methods of using a compound of formula II to treat certain symptoms of psoriasis, rheumatoid arthritis or multiple sclerosis.
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Page/Page column 16; 36
(2020/07/25)
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- 4-trifluoroacetyl-2-phenyloxazol-5-one: Versatile template for syntheses of trifluoromethylsubstituted heterocycles
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4-Trifluoroacetyl-2-phenyloxazol-5-one (1) is a versatile template for the synthesis of various trifluoromethyl-substituted heterocycles. Cyclocondesation of 1 with hydroxylamine and hydrazine afforded isoxazole and pyrazole, respectively. Another key protocol involves nucleophilic ring opening of 1 with H2O or MeOH to give a-amido trifluoromethyl ketones which are transformed into trifluoromethyl-substituted thiazoles, oxazoles, imidazoles, pyrazoles, and pyrimidines.
- Saijo, Ryosuke,Kurihara, Ken-Ichi,Kawase, Masami
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p. 2533 - 2553
(2014/01/06)
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- Efficient synthesis of (R)-3-amino-1,1,1-trifluoropropan-2-ol via a Dakin-West reaction followed by enantioselective reduction
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An efficient, chromatography-free asymmetric synthesis of (R)-3-amino-1,1,1-trifluoropropan-2-ol was developed for large scale production of a cholesterol ester transfer protein (CETP) inhibitor. The synthesis features a new efficient route to a β-amino trifluoromethylketone involving a modified Dakin-West reaction followed by an asymmetric hydrogenation or an enzymatic reduction of the resulting ketone to the alcohol.
- Wei, Lulin,Makowski, Teresa,Martinez, Carlos,Ghosh, Arun
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p. 2648 - 2651
(2009/04/07)
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- SYNTHESIS OF FLUORINATED α-AMINO KETONES PART I: α-BENZAMIDOALKYL MONO- DI- AND TRIFLUOROMETHYL KETONES
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2-Phenyl-5(4H)-oxazolones, obtained from α-amino acids, are reacted with di- and trifluoro acetic anhydride by a modified Dakin-West procedure to yield in a one-pot reaction α-benzamidoalkyl-di- and trifluoromethyl ketones in good yields.The monofluoromethyl analogues were also prepared from α-amino acids, however the use of the highly toxic fluoroacetic anhydride was avoided.The key step is the halogen exchange reaction on the corresponding bromomethyl ketone.
- Kolb, Michael,Barth, Jacqueline,Neises, Bernhard
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p. 1579 - 1582
(2007/10/02)
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