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Ma syntheses awa anali ma showtopper mu 2022

Njira 3 zosangalatsa zomwe akatswiri amapangira mankhwala chaka chino
ndi Bethany Halford

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ENzymes ZOPHUNZITSIDWA ZOPANGIDWA BIARYL BOND
Dongosolo lowonetsa kulumikizana kwa enzyme-catalyzed biaryl.
Akatswiri a zamankhwala amagwiritsa ntchito mamolekyu a biaryl, omwe ali ndi magulu a aryl omwe amamangiriridwa wina ndi mzake ndi mgwirizano umodzi, monga chiral ligands, zomangira zipangizo, ndi mankhwala.Koma kupanga biaryl motif yokhala ndi zitsulo zopangidwa ndi zitsulo, monga zolumikizirana za Suzuki ndi Negishi, nthawi zambiri zimafunikira njira zingapo zopangira kuti apange zibwenzi.Kuonjezera apo, machitidwe opangidwa ndi zitsulowa amalephera kupanga ma biaryls akuluakulu.Molimbikitsidwa ndi kuthekera kwa ma enzymes kuti ayambitse zochitika, gulu lotsogozedwa ndi Alison RH Narayan waku University of Michigan adagwiritsa ntchito chisinthiko cholunjika kupanga cytochrome P450 enzyme yomwe imapanga molekyulu ya biaryl kudzera pakuphatikizana kwa okosijeni kwa ma bond onunkhira a carbon-hydrogen.Enzymeyi imakwatiwa ndi mamolekyu onunkhira kuti apange stereoisomer imodzi mozungulira chomangira chotchinga chozungulira (chowonetsedwa).Ofufuzawo akuganiza kuti njira iyi ya biocatalytic ikhoza kukhala kusintha kwa mkate ndi batala popanga ma biaryl bond (Nature 2022, DOI: 10.1038/s41586-021-04365-7).

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Mphikidwe WA TERTIARY AMINES WODALIRA PA MCHEWWE WANG'ONO
Scheme ikuwonetsa zomwe zimapanga ma amines apamwamba kuchokera ku sekondale.
Kusakaniza zopangira zitsulo zokhala ndi ma elekitironi ndi ma amine olemera ma elekitironi nthawi zambiri zimapha zoyambitsa, kotero kuti zopangira zitsulo sizingagwiritsidwe ntchito pomanga ma amine apamwamba kuchokera ku ma amine achiwiri.M. Christina White ndi anzake a pa yunivesite ya Illinois Urbana-Champaign anazindikira kuti akhoza kuthana ndi vutoli ngati atawonjezera zokometsera zamchere ku maphikidwe awo a reactant.Posintha ma amine achiwiri kukhala amchere ammonium, akatswiri adapeza kuti amatha kuchitapo kanthu ndi mankhwalawa ndi ma terminal olefins, oxidant, ndi palladium sulfoxide catalyst kuti apange myriad tertiary amines ndi magulu osiyanasiyana ogwira ntchito (chitsanzo chawonetsedwa).Akatswiri a zamankhwala adagwiritsa ntchito zomwe adachita kuti apange mankhwala oletsa antipsychotic Abilify ndi Semap ndikusintha mankhwala omwe alipo omwe ndi ma amine achiwiri, monga antidepressant Prozac, kukhala ma amine apamwamba, kuwonetsa momwe akatswiri amapangira mankhwala atsopano kuchokera omwe alipo (Sayansi 2022, DOI: 10.1126/science.abn8382).

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AZAARENES ANAPANGIDWA CARBON CONTRACTION
Chiwembu chikuwonetsa quinoline N-oxide atasinthidwa kukhala N-acylindole.
Chaka chino akatswiri a zamankhwala anawonjezera ku repertoire ya kusintha kwa ma molekyulu, omwe ndi machitidwe omwe amasintha pakati pa mamolekyu ovuta.Muchitsanzo chimodzi, ofufuza adapanga kusintha komwe kumagwiritsira ntchito kuwala ndi asidi kuti adule carbon imodzi kuchokera mu azaarenes asanu ndi limodzi mu quinoline N-oxides kupanga N-acylindoles yokhala ndi mphete zisanu (chitsanzo chasonyezedwa).Zimene anachita, zimene akatswiri a zamankhwala a m’gulu la Mark D. Levin a ku yunivesite ya Chicago anachita, zimachokera pa zimene zinakhudza nyali ya mercury, yomwe imayatsa utali wosiyanasiyana wa kuwala.Levin ndi anzake anapeza kuti kugwiritsa ntchito kuwala-emitting diode kuti zimatulutsa kuwala pa 390 nm anawapatsa kulamulira bwino ndi kuwalola kupanga anachita ambiri quinoline N-oxides.Zomwe zatsopanozi zimapatsa opanga mamolekyu njira yosinthira ma cores azinthu zovuta ndipo zitha kuthandiza akatswiri azamankhwala omwe akufuna kukulitsa malaibulale awo omwe akufuna kugwiritsa ntchito mankhwala osokoneza bongo (Science 2022, DOI: 10.1126/science.abo4282).


Nthawi yotumiza: Dec-19-2022