• isibhengezo_sekhasi

Lawa ma-syntheses ayengama-showstopper ngo-2022

Izindlela ezi-3 ezithokozisayo osokhemisi abakhe izinhlanganisela kulo nyaka
nguBethany Halford

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AMA-ENCYMES AVELA AMABONDI E-BIARYL
Uhlelo olubonisa ukuhlangana kwe-enzyme-catalyzed biaryl.
Osokhemisi basebenzisa ama-molecule e-biaryl, ahlanganisa amaqembu e-aryl ahlanganiswe elinye nelinye ngesibopho esisodwa, njengama-chiral ligands, amabhlogo wokwakha wezinto zokwakha, kanye nemithi.Kodwa ukwenza i-biaryl motif ngokusabela okwenziwe nge-metal-catalyzed, okufana nokuhlangana kwe-Suzuki ne-Negishi, ngokuvamile kudinga izinyathelo ezimbalwa zokwenziwa zokwenza ozakwethu bokuhlanganisa.Ngaphezu kwalokho, lokhu kusabela kwe-metal-catalyzed kuyantengantenga lapho kwenziwa ama-biaryl amakhulu.Ligqugquzelwe ikhono lama-enzyme lokugqugquzela ukusabela, ithimba eliholwa u-Alison RH Narayan wase-University of Michigan lisebenzise ukuziphendukela kwemvelo okuqondisiwe ukuze lenze i-cytochrome P450 enzyme eyakha i-molecule ye-biaryl ngokuhlanganisa i-oxidative yamabhondi e-carbon-hydrogen anephunga elimnandi.I-enzyme ihlanganisa ama-molecule anephunga elimnandi ukuze idale isitiriyo esisodwa esizungeze isibopho esinokuzungezisa okuvinjiwe (okubonisiwe).Abacwaningi bacabanga ukuthi le ndlela ye-biocatalytic ingaba ukuguqulwa kwesinkwa nebhotela ekwenzeni amabhondi e-biaryl (Nature 2022, DOI: 10.1038/s41586-021-04365-7).

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IREsiphi ELAMA-AMINE ASEKUPHAKAMENI ATHEMBEKILE KUSAWOTI OMNCANE
Uhlelo lukhombisa ukusabela okwenza ama-amine emfundo ephakeme asuka kwesesibili.
Ukuxuba ama-electron-lambe metal catalysts nama-electron-rich rich amines ngokuvamile kubulala ama-catalysts, ngakho-ke ama-reagents ensimbi awakwazi ukusetshenziselwa ukwakha ama-amine aphakeme asuka kuma-amine esibili.M. Christina White nozakwabo eNyuvesi yase-Illinois Urbana-Champaign babone ukuthi bangakwazi ukubhekana nale nkinga uma bengeza isinongo esinosawoti kuresiphi yabo esabelayo.Ngokuguqula ama-amine esibili abe usawoti we-ammonium, osokhemisi bathola ukuthi bangasabela lezi zinhlanganisela nge-olefin yokugcina, i-oxidant, kanye ne-palladium sulfoxide catalyst ukuze bakhe inqwaba yama-amine emfundo ephakeme ngamaqembu ahlukahlukene asebenzayo (isibonelo esibonisiwe).Osokhemisi basebenzise ukusabela ukwenza imishanguzo ye-antipsychotic i-Abilify ne-Semap kanye nokuguqula izidakamizwa ezikhona ezingama-amine esibili, njenge-Prozac eqeda ukucindezeleka, zibe ama-amine aphezulu, okubonisa ukuthi osokhemisi bangayenza kanjani imithi emisha ngalezo ezikhona (Isayensi 2022, DOI: 10.1126/science.abn8382).

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I-AZAARENES IKHISHWA NGENKONKELELO YEKHABONI
Uhlelo lubonisa i-quinoline N-oxide eguqulelwe ku-N-acylindole.
Kulo nyaka osokhemisi banezele embhalweni wokuhlela wamangqamuzana, okuwukusabela okwenza izinguquko kuma-cores ama-molecule ayinkimbinkimbi.Esibonelweni esisodwa, abacwaningi bathuthukise uguquko olusebenzisa ukukhanya ne-asidi ukusika ikhabhoni eyodwa kuma-azaarene anamalungu ayisithupha ku-quinoline N-oxides ukuze kwakheke i-N-acylindoles enamasongo anamalungu amahlanu (isibonelo esibonisiwe).Ukusabela, okwasungulwa osokhemisi eqenjini lika-Mark D. Levin e-University of Chicago, kusekelwe ekuphenduleni okuhilela isibani se-mercury, esikhipha amaza okukhanya amaningi.U-Levin nozakwabo bathola ukuthi ukusebenzisa i-diode ekhipha ukukhanya ekhipha ukukhanya ku-390 nm kwabanika ukulawula okungcono futhi kwabavumela ukuthi benze ukusabela okuvamile kuma-quinoline N-oxides.Ukusabela okusha kunikeza abenzi be-molecule indlela yokulungisa kabusha ama-cores we-compounds eyinkimbinkimbi futhi kungasiza osokhemisi bezokwelapha abafuna ukukhulisa imitapo yolwazi yabo yezidakamizwa (Isayensi 2022, DOI: 10.1126/science.abo4282).


Isikhathi sokuthumela: Dec-19-2022