3 txoj kev zoo siab uas cov kws tshuaj tsim cov tshuaj sib xyaw xyoo no
los ntawm Bethany Halford
Cov ENZYMES uas tau tsim los ntawm BIARYL BOND
Daim duab qhia txog kev sib txuas ntawm biaryl uas muaj enzyme-catalyzed.
Cov kws tshuaj siv cov biaryl molecules, uas muaj cov pab pawg aryl khi rau ib leeg los ntawm ib qho kev sib txuas, ua chiral ligands, cov khoom siv tsim, thiab cov tshuaj. Tab sis ua rau cov biaryl motif nrog cov tshuaj tiv thaiv hlau, xws li Suzuki thiab Negishi cross-couplings, feem ntau xav tau ntau kauj ruam synthetic los ua cov khub sib txuas. Ntxiv mus, cov tshuaj tiv thaiv hlau no tsis ua haujlwm thaum ua cov biaryls loj. Tau txais kev tshoov siab los ntawm lub peev xwm ntawm cov enzymes los ua kom cov tshuaj tiv thaiv, ib pab neeg coj los ntawm University of Michigan's Alison RH Narayan siv kev hloov pauv los tsim cov enzyme cytochrome P450 uas tsim cov biaryl molecule los ntawm kev sib txuas oxidative ntawm cov carbon-hydrogen bonds aromatic. Cov enzyme sib txuas cov aromatic molecules los tsim ib qho stereoisomer nyob ib puag ncig cov ntawv cog lus nrog kev tig tsis zoo (qhia). Cov kws tshawb nrhiav xav tias txoj hauv kev biocatalytic no yuav dhau los ua kev hloov pauv yooj yim rau kev ua cov biaryl bonds (Nature 2022, DOI: 10.1038/s41586-021-04365-7).
DAIM NTAWV QHIA TXOG TERTIARY AMINES UAS SIV ME NTSEEG NTSEV
Daim duab qhia txog kev ua haujlwm uas ua rau cov amines tertiary los ntawm cov amines theem nrab.
Kev sib xyaw cov tshuaj catalysts hlau uas muaj electron ntau nrog cov amines uas muaj electron ntau feem ntau tua cov catalysts, yog li cov tshuaj reagents hlau tsis tuaj yeem siv los tsim cov amines tertiary los ntawm cov amines secondary. M. Christina White thiab cov npoj yaig ntawm University of Illinois Urbana-Champaign tau paub tias lawv tuaj yeem daws qhov teeb meem no yog tias lawv ntxiv qee cov txuj lom ntsev rau lawv cov tshuaj reactant. Los ntawm kev hloov cov amines secondary mus rau hauv cov ntsev ammonium, cov kws tshuaj pom tias lawv tuaj yeem ua cov tshuaj no nrog cov terminal olefins, ib qho oxidant, thiab cov catalyst palladium sulfoxide los tsim ntau cov tertiary amines nrog ntau yam pab pawg ua haujlwm (piv txwv qhia). Cov kws tshuaj siv cov tshuaj no los ua cov tshuaj antipsychotic Abilify thiab Semap thiab hloov cov tshuaj uas twb muaj lawm uas yog cov amines secondary, xws li cov tshuaj antidepressant Prozac, mus rau hauv cov amines tertiary, qhia txog yuav ua li cas cov kws tshuaj yuav ua cov tshuaj tshiab los ntawm cov uas twb muaj lawm (Science 2022, DOI: 10.1126/science.abn8382).
AZAARENES TAU TXAIS KEV COMBINATION
Daim duab qhia txog quinoline N-oxide hloov pauv mus ua N-acylindole.
Xyoo no cov kws tshuaj tau ntxiv rau hauv cov repertoire ntawm kev kho molecular, uas yog cov tshuaj tiv thaiv uas ua rau muaj kev hloov pauv rau cov cores ntawm cov molecules nyuaj. Hauv ib qho piv txwv, cov kws tshawb fawb tau tsim kev hloov pauv uas siv lub teeb thiab kua qaub los txiav ib qho carbon tawm ntawm rau-membered azaarenes hauv quinoline N-oxides los tsim N-acylindoles nrog tsib-membered rings (piv txwv qhia). Cov tshuaj tiv thaiv, tsim los ntawm cov kws tshuaj hauv Mark D. Levin pawg ntawm University of Chicago, yog raws li cov tshuaj tiv thaiv uas cuam tshuam nrog lub teeb mercury, uas tso tawm ntau lub wavelengths ntawm lub teeb. Levin thiab cov npoj yaig pom tias kev siv lub teeb-emitting diode uas tso tawm lub teeb ntawm 390 nm tau muab rau lawv tswj hwm zoo dua thiab tso cai rau lawv ua cov tshuaj tiv thaiv dav dav rau quinoline N-oxides. Cov tshuaj tiv thaiv tshiab muab rau cov neeg tsim molecule ib txoj hauv kev los kho dua tshiab cov cores ntawm cov tshuaj sib xyaw thiab tuaj yeem pab cov kws tshuaj kho mob nrhiav kev nthuav lawv cov tsev qiv ntawv ntawm cov neeg sib tw tshuaj (Science 2022, DOI: 10.1126/science.abo4282).
Lub sijhawm tshaj tawm: Lub Kaum Ob Hlis-19-2022