• iphepha_ibhena

Ezi syntheses beziyi-showstoppers ngo-2022

Iindlela ezi-3 ezichulumancisayo ezithe iikhemisti zakha iikhompawundi kulo nyaka
nguBethany Halford

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IIENNZYM EZAKHIWEYO ZE-BIARYL BODS
Inkqubo ebonisa i-enzyme-catalyzed biaryl coupling.
Iikhemisti zisebenzisa iimolekyuli ze-biaryl, ezibonisa amaqela e-aryl adityaniswe omnye komnye ngebhondi enye, njenge-chiral ligands, iibhloko zokwakha, kunye namayeza.Kodwa ukwenza i-biaryl motif nge-metal-catalyzed reactions, njengeSuzuki kunye ne-Negishi cross-couplings, ngokuqhelekileyo kufuna amanyathelo amaninzi okwenziwa ukwenza amaqabane okudibanisa.Ngaphezu koko, ezi mpendulo zentsimbi-catalyzed ziyadodobala xa kusenziwa i-biaryls enkulu.Iphenjelelwe kukukwazi kwee-enzymes ukuvuselela ukusabela, iqela elikhokelwa yiYunivesithi yaseMichigan's Alison RH Narayan lisebenzise indaleko ethe ngqo ukwenza i-cytochrome P450 enzyme eyakha imolekyuli ye-biaryl ngokudityaniswa kwe-oxidative yebhondi ye-carbon-hydrogen enevumba elimnandi.I-enzayimu itshata iimolekyuli ezinevumba elimnandi ukuze zenze i-stereoisomer enye ejikeleze iqhina ngokujikeleza okuthintelweyo (okubonisiwe).Abaphandi bacinga ukuba le ndlela ye-biocatalytic ingaba yinguqu yesonka kunye nebhotela yokwenza iibhondi ze-biaryl (Indalo 2022, i-DOI: 10.1038 / s41586-021-04365-7).

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IREsiphi ye-TERTIARY AMINES IXHOMEKE KWITYUWA ENGCANE
Inkqubo ibonisa impendulo eyenza i-amines yamabanga aphakamileyo ukusuka kweyesibini.
Ukuxuba i-electron-elambileyo i-metal catalysts kunye ne-electron-rich amines ngokuqhelekileyo ibulala ii-catalysts, ngoko ke ii-reagents zetsimbi azinakusetyenziselwa ukwakha i-amines yamabanga aphakamileyo ukusuka kwi-amines yesibini.M. Christina White kunye noogxa babo kwiYunivesithi yase-Illinois Urbana-Champaign baqaphela ukuba bangakwazi ukujamelana nale ngxaki ukuba bongeze isinongo esinetyuwa kwiresiphi yabo yokusabela.Ngokuguqula i-amines yesibini ibe ziityuwa ze-ammonium, iikhemikhali zafumanisa ukuba ziyakwazi ukusabela ezi zixhobo kunye ne-terminal olefins, i-oxidant, kunye ne-palladium sulfoxide catalyst ukudala i-myriad tertiary amines kunye namaqela ahlukeneyo asebenzayo (umzekelo ubonisiwe).Oosokhemisti basebenzise impendulo ukwenza amayeza e-antipsychotic abe-Abilify kunye ne-Semap kunye nokuguqula amachiza asele ekhona azii-amines zesibini, njenge-antidepressant Prozac, zibe zii-amines eziphezulu, ezibonisa ukuba iikhemisti zinokuwenza njani amachiza amatsha kulawo sele ekhona (iSayensi 2022, DOI: 10.1126/science.abn8382).

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I-AZAARENES YAYENZA INKONKELELO YEKHABHNINI
Inkqubo ibonisa i-quinoline N-oxide eguqulelwe kwi-N-acylindole.
Kulo nyaka iikhemisti zongezelele kwirepertoire yokuhlelwa kweemolekyuli, eziziimpendulo ezenza utshintsho kwiicores zeemolekyuli ezintsonkothileyo.Komnye umzekelo, abaphandi baye benza inguqu esebenzisa ukukhanya kunye ne-asidi ukusika i-carbon enye ngaphandle kwe-azaarenes enamalungu amathandathu kwi-quinoline N-oxides ukwenza i-N-acylindoles kunye nezangqa ezingamalungu amahlanu (umzekelo ubonisiwe).Indlela abasabela ngayo, eyaveliswa ngoosokhemesti kwiqela likaMark D. Levin kwiYunivesithi yaseChicago, isekelwe kwintsabelo eyayibandakanya isibane semercury, esikhupha amaza okukhanya amaninzi.U-Levin kunye noogxa bafumanisa ukuba ukusebenzisa i-diode ekhupha ukukhanya ekhupha ukukhanya kwi-390 nm yabanika ulawulo olungcono kwaye yabavumela ukuba benze ukusabela ngokubanzi kwi-quinoline N-oxides.I-reaction entsha inika abenzi be-molecule indlela yokulungisa ii-cores ze-compounds eziyinkimbinkimbi kwaye inokunceda iikhemisti zamayeza zijonge ukwandisa iilayibrari zabo zabaviwa beziyobisi (iSayensi 2022, i-DOI: 10.1126 / science.abo4282).


Ixesha lokuposa: Dec-19-2022