- Enantioselective, Catalytic Vicinal Difluorination of Alkenes
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The enantioselective, catalytic vicinal difluorination of alkenes is reported by II/IIII catalysis using a novel, C2-symmetric resorcinol derivative. Catalyst turnover via in situ generation of an ArIIIIF2 species is enabled by Selectfluor oxidation and addition of an inexpensive HF–amine complex. The HF:amine ratio employed in this process provides a handle for regioselective orthogonality as a function of Br?nsted acidity. Selectivity reversal from the 1,1-difluorination pathway (geminal) to the desired 1,2-difluorination (vicinal) is disclosed (>20:1 in both directions). Validation with electron deficient styrenes facilitates generation of chiral bioisosteres of the venerable CF3 unit that is pervasive in drug discovery (20 examples, up to 94:06 e.r.). An achiral variant of the reaction is also presented using p-TolI (up to >95 % yield).
- Scheidt, Felix,Sch?fer, Michael,Sarie, Jér?me C.,Daniliuc, Constantin G.,Molloy, John J.,Gilmour, Ryan
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p. 16431 - 16435
(2018/11/23)
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- CARBAZOLE COMPOUNDS AND METHODS OF USING SAME
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The present invention provides carbazole compounds of the formula (I), which can be used for treating microbial, protozoan, viral infections and cancer. ?
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Paragraph 00137
(2015/02/25)
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- Methods For The Treatment of Central Nervous System Tumors
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Methods for the treatment of primary and secondary central nervous system tumors in a mammal which comprise administration of a benzimidazole thiophene compound are provided.
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- para-Formylation of nitroarenes via vicarious nucleophilic substitution of hydrogen with tris(benzotriazol-1-yl)methane
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Reaction of nitroarenes 1 with tris(benzotriazol-1-yl)methyl 2 anion afforded para-bis(benzotriazol-1-yl)methylated products 3 which, upon treatment with zinc bromide and hydrochloric acid, yielded the corresponding p-nitroarylaldehydes 4 in good yields.
- Katritzky, Alan R.,Xie, Linghong
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p. 347 - 350
(2007/10/02)
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- Ortho-nitro-promoted Ullmann ether synthesis : Application in the syntheses of K-13 and the isodityrosine unit of vancomycin
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A nitro group in the ortho-position of the aryl halide component facilitates Ullmann ether synthesis for the syntheses of all isodityrosine units present in wide variety of natural products, first time, on the basis of a common strategy.
- Rama Rao,Chakraborty,Laxma Reddy,Srinivasa Rao
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p. 4799 - 4802
(2007/10/02)
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