- Photoenzymatic Generation of Unstabilized Alkyl Radicals: An Asymmetric Reductive Cyclization
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Flavin-dependent "ene"-reductases can generate stabilized alkyl radicals when irradiated with visible light; however, they are not known to form unstabilized radicals. Here, we report an enantioselective radical cyclization using alkyl iodides as precursors to unstabilized nucleophilic radicals. Evidence suggests this species is accessed by photoexcitation of a charge-transfer complex that forms between flavin and substrate within the protein active site. Stereoselective delivery of a hydrogen atom from the flavin semiquinone to the prochiral radical formed after cyclization provides high levels of enantioselectivity across a variety of substrates. Overall, this transformation demonstrates that photoenzymatic catalysis can address long-standing selectivity challenges in the radical literature.
- Clayman, Phillip D.,Hyster, Todd K.
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p. 15673 - 15677
(2020/10/18)
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- BIARYL PYRAZOLES AS NRF2 REGULATORS
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The present invention relates to biaryl pyrazole compounds, methods of making them, pharmaceutical compositions containing them and their use as NRF2 regulators.
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Page/Page column 451
(2017/08/01)
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- NRF2 REGULATORS
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Provided are aryl analogs,pharmaceutical compositions containing them and their use as NRF2 regulators.
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Page/Page column 346
(2017/01/02)
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- COMPOUNDS USEFUL AS MODULATORS OF TRPM8
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The present invention includes compounds useful as modulators of TRPM8, such as compounds of Formulae (Ia), (Ib) and (Ic), and the subgenus and species thereof; personal products containing those compounds; and the use of those compounds and the personal products, particularly the use of increasing or inducing chemesthetic sensations, such as cooling or cold sensations.
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Paragraph 0894
(2016/03/29)
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- Conjugate Addition Reactions Mediated by Samarium(II) Iodide
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Samarium(II) iodide in conjunction with a catalytic low-valent transition metal species has been employed to promote the conjugate addition reaction of primary and secondary alkyl halides onto α,β-unsaturated esters and amides. The method has been determined to be quite general and hence has been extended to the cyclization reactions of alkyl halides onto α,β-unsaturated lactones, lactams, and nitriles. The cyclization reactions described herein provide a very general approach to the synthesis of functionalized carbocycles from simple acyclic precursors with excellent diastereoselectivity and under very mild reaction conditions.
- Molander, Gary A.,Harris, Christina R.
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p. 7418 - 7429
(2007/10/03)
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- Perfumery composition comprising 2-cyclohexylpropionic acid or its derivative
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Disclosed is a perfumery composition comprising a 2-cyclohexylpropionic acid or its derivative represented by the following formula (I): STR1 wherein R is a hydrogen atom, an alkyl group having 1-4 carbon atoms, or an alkenyl group having 2-4 carbon atoms. The compounds have a wide variety of odors and a wide application as perfumery compositions such as high-grade perfumery compositions, perfumes, soaps, shampoos, rinses, detergents, cosmetics, sprays, room fragrances, and the like.
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- O-SILYLATED ENOLATES IN ORGANIC SYNTHESIS: SULPHUR-MEDIATED ALKYLATION OF ESTERS WITH ALKENES.
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O-Silylated ester enolates can be alkylated, under ZnBr2-catalysis, by the PhSCl-adducts of mono- and di-substituted alkenes to give γ-phenylthioesters, from which sulphur can be removed both reductively and oxidatively.This alkene carbosulphenylation rea
- Patel, Shailesh K.,Paterson, Ian
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p. 1315 - 1318
(2007/10/02)
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