Pawg Cyano muaj zog polarity thiab electron absorption, yog li nws tuaj yeem mus tob rau hauv cov protein hom phiaj los tsim cov hydrogen bonds nrog cov amino acid residues tseem ceeb hauv qhov chaw ua haujlwm. Tib lub sijhawm, pawg cyano yog lub cev bioelectronic isosteric ntawm carbonyl, halogen thiab lwm cov pab pawg ua haujlwm, uas tuaj yeem txhim kho kev sib cuam tshuam ntawm cov tshuaj me me thiab cov protein hom phiaj, yog li nws tau siv dav hauv kev hloov kho cov qauv ntawm cov tshuaj thiab cov tshuaj tua kab [1]. Cov neeg sawv cev cyano uas muaj cov tshuaj kho mob suav nrog saxagliptin (Daim Duab 1), verapamil, febuxostat, thiab lwm yam; Cov tshuaj ua liaj ua teb suav nrog bromofenitrile, fipronil, fipronil thiab lwm yam. Tsis tas li ntawd, cov tshuaj cyano kuj muaj txiaj ntsig zoo rau kev siv hauv cov teb ntawm cov tshuaj tsw qab, cov ntaub ntawv ua haujlwm thiab lwm yam. Piv txwv li, Citronitrile yog cov tshuaj tsw qab nitrile tshiab thoob ntiaj teb, thiab 4-bromo-2,6-difluorobenzonitrile yog cov khoom siv raw tseem ceeb rau kev npaj cov khoom siv kua siv lead ua kua. Nws tuaj yeem pom tias cov tshuaj cyano tau siv dav hauv ntau qhov chaw vim lawv cov khoom tshwj xeeb [2].

Pawg Cyano muaj zog polarity thiab electron absorption, yog li nws tuaj yeem mus tob rau hauv cov protein hom phiaj los tsim cov hydrogen bonds nrog cov amino acid residues tseem ceeb hauv qhov chaw ua haujlwm. Tib lub sijhawm, pawg cyano yog lub cev bioelectronic isosteric ntawm carbonyl, halogen thiab lwm cov pab pawg ua haujlwm, uas tuaj yeem txhim kho kev sib cuam tshuam ntawm cov tshuaj me me thiab cov protein hom phiaj, yog li nws tau siv dav hauv kev hloov kho cov qauv ntawm cov tshuaj thiab cov tshuaj tua kab [1]. Cov neeg sawv cev cyano uas muaj cov tshuaj kho mob suav nrog saxagliptin (Daim Duab 1), verapamil, febuxostat, thiab lwm yam; Cov tshuaj ua liaj ua teb suav nrog bromofenitrile, fipronil, fipronil thiab lwm yam. Tsis tas li ntawd, cov tshuaj cyano kuj muaj txiaj ntsig zoo rau kev siv hauv cov teb ntawm cov tshuaj tsw qab, cov ntaub ntawv ua haujlwm thiab lwm yam. Piv txwv li, Citronitrile yog cov tshuaj tsw qab nitrile tshiab thoob ntiaj teb, thiab 4-bromo-2,6-difluorobenzonitrile yog cov khoom siv raw tseem ceeb rau kev npaj cov khoom siv kua siv lead ua kua. Nws tuaj yeem pom tias cov tshuaj cyano tau siv dav hauv ntau qhov chaw vim lawv cov khoom tshwj xeeb [2].

2.2 electrophilic cyanidation reaction ntawm enol boride
Kensuke Kiyokawa pab neeg [4] siv cov tshuaj cyanide reagents n-cyano-n-phenyl-p-toluenesulfonamide (NCTS) thiab p-toluenesulfonyl cyanide (tscn) kom ua tiav cov electrophilic cyanidation ntawm enol boron compounds (Daim Duab 3). Los ntawm txoj kev tshiab no, ntau yam β- Acetonitrile, thiab muaj ntau yam substrates.

2.3 cov tshuaj tiv thaiv organic catalytic stereoselective silico cyanide ntawm ketones
Tsis ntev los no, pab pawg neeg Benjamin [5] tau tshaj tawm hauv phau ntawv xov xwm Nature qhov kev sib txawv ntawm 2-butanone (Daim Duab 4a) thiab qhov kev sib xyaw ua ke ntawm 2-butanone nrog cov enzymes, cov organic catalysts thiab cov hlau hloov pauv catalysts, siv HCN lossis tmscn ua cyanide reagent (Daim Duab 4b). Nrog tmscn ua cyanide reagent, 2-butanone thiab ntau yam ketones tau raug rau cov tshuaj tiv thaiv silyl cyanide uas muaj enantioselective heev nyob rau hauv cov xwm txheej catalytic ntawm idpi (Daim Duab 4C).

Daim Duab 4 A, kev sib txawv ntawm enantiomeric ntawm 2-butanone. b. Asymmetric cyanidation ntawm 2-butanone nrog cov enzymes, cov organic catalysts thiab cov hlau hloov pauv catalysts.
c. Idpi ua rau muaj kev cuam tshuam ntau ntawm 2-butanone thiab ntau yam ketones.
2.4 kev txo qis cyanidation ntawm aldehydes
Hauv kev tsim cov khoom ntuj, cov tshuaj ntsuab tosmic yog siv los ua cov tshuaj cyanide reagent kom yooj yim hloov cov aldehydes uas raug cuam tshuam rau hauv nitriles. Txoj kev no ntxiv rau kev qhia txog cov pa roj carbon ntxiv rau hauv aldehydes thiab ketones. Txoj kev no muaj qhov tseem ceeb hauv Enantiospecific tag nrho cov tshuaj jiadifenolide thiab yog ib kauj ruam tseem ceeb hauv kev tsim cov khoom ntuj, xws li kev tsim cov khoom ntuj xws li clerodane, caribenol A thiab caribenol B [6] (Daim Duab 5).

2.5 electrochemical cyanide tshuaj tiv thaiv ntawm cov organic amine
Ua ib qho kev siv tshuab ua kom ntsuab, cov organic electrochemical synthesis tau siv dav hauv ntau qhov chaw ntawm cov organic synthesis. Nyob rau hauv xyoo tas los no, ntau thiab ntau tus kws tshawb fawb tau them sai sai rau nws. PrashanthW. Menezes pab pawg [7] nyuam qhuav tshaj tawm tias aromatic amine lossis aliphatic amine tuaj yeem ncaj qha oxidized rau cov cyano sib xws hauv 1m KOH kua (tsis ntxiv cyanide reagent) nrog lub peev xwm tas mus li ntawm 1.49vrhe siv cov catalyst Ni2Si pheej yig, nrog cov txiaj ntsig siab (Daim Duab 6).

03 cov ntsiab lus luv luv
Cyanidation yog ib qho tseem ceeb heev rau kev tsim cov organic. Pib los ntawm lub tswv yim ntawm kev tshuaj ntsuab ntsuab, cov tshuaj cyanide reagents uas zoo rau ib puag ncig yog siv los hloov cov tshuaj lom thiab cov tshuaj cyanide reagents ib txwm muaj, thiab cov txheej txheem tshiab xws li cov tshuaj tsis muaj kuab tshuaj, tsis muaj catalytic thiab microwave irradiation yog siv los nthuav dav ntxiv qhov ntau thiab qhov tob ntawm kev tshawb fawb, yog li ntawd thiaj li tsim tau cov txiaj ntsig loj hauv kev lag luam, kev sib raug zoo thiab ib puag ncig hauv kev tsim khoom lag luam [8]. Nrog rau kev nce qib tas mus li ntawm kev tshawb fawb, cov tshuaj cyanide yuav tsim mus rau qhov muaj txiaj ntsig zoo, kev lag luam thiab tshuaj ntsuab.
Lub sijhawm tshaj tawm: Cuaj hlis-07-2022




