- Synthesis of Alkylated Pyrimidines via Photoinduced Coupling Using Benzophenone as a Mediator
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The synthesis of alkylated pyrimidines was achieved via benzophenone-mediated photoinduced coupling between saturated heterocycles and sulfonylpyrimidines. The pyrimidine ring was selectively introduced at the nonacidic C(sp3)-H bond proximal to heteroatoms including oxygen, nitrogen, and sulfur. This is a coupling reaction mediated solely by photoexcited benzophenone, an organic molecule, without the aid of any metallic catalysts or reagents.
- Kamijo, Shin,Kamijo, Kaori,Murafuji, Toshihiro
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p. 2664 - 2671
(2017/03/14)
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- Regioselective 2-Amination of Polychloropyrimidines
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The regioselective amination of substituted di- and trichloropyrimidines affording the 2-substituted products is reported. While aryl- and heteroarylamines require the use of a dialkylbiarylphosphine-derived palladium catalyst for high efficiency, more nucleophilic dialkylamines produce 2-aminopyrimidines under noncatalyzed SNAr conditions. The key is the use of 5-trimethylsilyl-2,4-dichloropyrimidine as a surrogate for the parent dichloropyrimidine. For more challenging cases, the 2-chloro-4-thiomethoxy analogues were prepared and exclusively afford the desired 2-aminated-4-thiomethoxypyrimidine products.
- Smith, Sean M.,Buchwald, Stephen L.
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supporting information
p. 2180 - 2183
(2016/06/01)
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- QUINOLINONE PYRIMIDINES COMPOSITIONS AS MUTANT-ISOCITRATE DEHYDROGENASE INHIBITORS
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The invention relates to inhibitors of mutant isocitrate dehydrogenase (mt-IDH) proteins with neomorphic activity useful in the treatment of cell-proliferation disorders and cancers, having the Formula: where A, B, W1, W2, W3, and R1-R6 are described herein.
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Paragraph 0841-0843
(2016/04/19)
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- SUBSTITUTED PYRIMIDINE COMPOUNDS AND THEIR USE AS SYK INHIBITORS
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Compounds of Formula (I) and methods for inhibiting kinases, including spleen tyrosine kinases, are disclosed. Also disclosed are methods for treating a kinase-mediated disease or condition by administering to a subject a therapeutically effective amount of the compound of Formula (I).
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Page/Page column 63
(2013/07/31)
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- Synthesis and herbicidal activity of 2-(3-(trifluoromethyl)-5-(alkoxy)-1H- pyrazol-1-yl)-4-aryloxypyrimidine derivatives
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(Chemical Equation Presented) A series of 2-(3-(trifluoromethyl)-5-(alkoxy) -1H-pyrazol-l-yl)-4-aryloxypyrimidine derivatives were designed and synthesized. The structures of all the title compounds were confirmed by 1H NMR and elementary analy
- Liu, Wei-Min,Zhu, You-Quan,Wang, Yi-Feng,Liu, Bin,Zou, Xiao-Mao,Yang, Hua-Zheng
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p. 967 - 971
(2008/03/29)
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- Mixed Mg/Li amides of the type R2NMgCl·LiCl as highly efficient bases for the regioselective generation of functionalized aryl and heteroaryl magnesium compounds
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(Chemical Equation Presented) Two are better than one: Mixed lithium-magnesium complexes of the type R2NMgCl·LiCl are kinetically highly active bases that convert a range of polyfunctional aromatic and heteroaromatic substrates into the corresponding magnesiated derivatives with high regioselectivity.
- Krasovskiy, Arkady,Krasovskaya, Valeria,Knochel, Paul
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p. 2958 - 2961
(2007/10/03)
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