- A high-yielding protocol for the synthesis of 4,5-diarylpyrimidin-2-amine derivatives from chalcones
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A novel, high yielding and versatile protocol was achieved for the synthesis of 4,5-diaryl-2-pyrimidinamine derivatives from chalcones. The synthesis was accomplished by converting the chalcones into 3-chloro-2,3-diaryl-2-propen-1-ones followed by subsequent reaction with amidine derivatives.
- Kooramatom Unni, Krishnaraj,Menon, Prasanth K.,George, Scholly Clair,Thomas, Sajesh P.,Devaky
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p. 112 - 118
(2021/10/07)
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- Metal-free, one-pot, sequential protocol for transforming ,-epoxy ketones to -hydroxy ketones and -methylene ketones
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A new sequential, one-pot protocol for transforming 1,3-disubstituted 2,3-epoxy ketones to β;-hydroxy ketones and α-methylene ketones has been developed. Reaction of epoxy ketones with boron trifluoride etherate (BF3·OEt2) generates the cationic intermediates by regioselective epoxide ring opening and an acyl shift. Then, a treatment of these cations with 2-aryl-1,3-dimethylbenzimidazolines (DMBIH) results in formation of 1,2-disubstituted 3-hydroxy ketones. DMBIH serves as a hydride donor in the second step of this process. Finally, the β;-hydroxy ketones can be converted to 1,2-disubstituted 2-methylene ketones by treatment with methanesulfonic acid or a combination of methanesulfonyl chloride and triethylamine. Importantly, the sequential steps involved in formation of the α-methylene ketone products can be carried out in one pot.
- Hasegawa, Eietsu,Arai, Saki,Tayama, Eiji,Iwamoto, Hajime
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p. 1593 - 1600
(2015/02/19)
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