- Convergent Synthesis of PI3K Inhibitor GDC-0908 Featuring Palladium-Catalyzed Direct C-H Arylation toward Dihydrobenzothienooxepines
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A practical convergent synthesis of PI3K inhibitor GDC-0908 (1) is described. The process features a dihydrobenzothienooxepine formation via palladium-catalyzed intramolecular direct C-H arylation and a Negishi coupling to construct the key C-C bonds. We
- Zhang, Haiming,Li, Beryl X.,Wong, Brian,Stumpf, Andreas,Sowell, C. Gregory,Gosselin, Francis
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p. 4796 - 4802
(2019/04/30)
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- HETEROCYCLIC COMPOUNDS AS PESTICIDES
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The present application relates to novel heterocyclic compounds, to the use thereof for controlling animal pests including arthropods, insects and nematodes, and to processes and intermediates for preparation of the novel compounds.
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Paragraph 0464; 0465; 0466
(2017/08/01)
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- Facile synthesis of 3-amino-5-aryl-1,2,4-oxadiazoles: Via PIDA-mediated intramolecular oxidative cyclization
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A mild and efficient method for the synthesis of 3-amino-5-aryl-1,2,4-oxadiazole by intramolecular cyclization using PhI(OAc)2 (PIDA) as an oxidant is developed. Various 3-amino-5-aryl-1,2,4-oxadiazoles are prepared in moderate to good yields,
- Lu, Kuan,Duan, Liancheng,Xu, Boxuan,Yin, Weile,Wu, Di,Zhao, Yanfang,Gong, Ping
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p. 54277 - 54280
(2016/07/06)
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- NOVEL THERAPEUTIC COMPOUNDS
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Disclosed herein are novel compounds of Formula (I), wherein the variables are defined as herein. The compounds of Formula (I) are useful as kinase inhibitors and as such would be useful in treating certain conditions and diseases, especially inflammatory conditions and diseases as well as proliferative disorders such as cancer.
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Page/Page column 163
(2009/03/07)
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- A generalized synthesis of 3-amino-5-aryl-, 3-amino-5-polyfluorophenyl-, and 3-amino-5-alkyl-1,2,4-oxadiazoles through ring-degenerate rearrangements
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A generalized synthesis of 3-amino-5-aryl-, 3-amino-5-polyfluorophenyl- and 3-amino-5-alkyl-1,2,4-oxadiazoles has been developed starting from the 3-amino-5-methyl-1,2,4-oxadiazole as a common synthon. Aroylation or alkanoylation of this aminooxadiazole,
- Buscemi, Silvestre,Pace, Andrea,Frenna, Vincenzo,Vivona, Nicolo?
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p. 811 - 823
(2007/10/03)
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- PHOTOCHEMICAL BEHAVIOUR OF 1,2,5-OXADIAZOLES - IRRADIATION OF SOME 3-ACYLAMINO-1,2,5-OXADIAZOLES IN THE PRESENCE OF NUCLEOPHILES
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The photochemical behaviour of some 3-acylamino-1,2,5-oxadiazoles (furazans) has been investigated.On irradiation at 254 nm in the presence of nucleophiles (ammonia, primary or secondary amines), the photoreaction produced 3-substituted 1,2,3-oxadiazoles in which the substituent at C(3) arises from the used reagent.Some mechanistic considerations are reported.
- Buscemi, Silvestre,Frenna, Vincenzo,Caronna, Tullio,Vivona, Nicolo
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p. 2313 - 2322
(2007/10/02)
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- Heterocyclic Rearrangements: Rearrangement of N-(1,2,4-Oxadiazol-3-yl)-β-enamino Ketones into Pyrimidine N-Oxides
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The behaviour of N-(5-R-1,2,4-oxadiazol-3-yl)-β-enamino ketones towards rearrangement has been investigated.In the presence of anionic reagents in ethanol solution, they rearrange to pyrimidine N-oxides.The synthesis and hydrolytic ring opening of a oxadiazolopyrimidinium system is also reported.
- Vivona, Nicolo,Buscemi, Silvestre,Frenna, Vincenzo,Ruccia, Michele
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