Leamisole hmoov, molecular formula c11h12n2s, CAS 14769-73-4, paub meej molecular hnyav tus nqi ntawm 204.291 g / molis tau hloov kho me ntsis ntawm cov dej crystal lossis ntsev. Nws cov tsos yog tus dawb kom tawm dawb crystalline hmoov, tsw tsw tab sis iab tab sis iab hauv saj. Cov xeeb ceem no yuav tsum tau npog los ntawm txheej thev naus laus zis hauv kev txhim kho cov qauv los npog qhov ncauj tsis zoo saj. Nyob rau hauv cov nqe lus ntawm cov qauv siv lead ua, nws nthuav tawm rab koob li cas los yog Crystalline ntau ntawm 230-239 Qib C), Qhia Txog Kev Nyuaj Siab Thermal Stability. Nws yog ib qho kev ua yeeb yam zoo tshaj plaws dav-speworming tshuaj uas kuj muaj immunomodulatory. Nws yog tsuas yog siv rau kev kho mob ntawm cov hnyuv nematworm thiab woldworm) thiab tuaj yeem siv ua cov tshuaj tiv thaiv kab mob rau kev tiv thaiv kab mob sib kis. Nws cov kev ua tshuab ntawm kev ua haujlwm suav nrog inhibiting kev ua si ntawm parasendic enzymes, thaum txhim kho txoj haujlwm ntawm t lymphocytes thiab macropholages.
Cov ntaub ntawv ntxiv ntawm kev sib txuas lus:
Peb Cov Khoom
Levamisole +. coa
Leamisole hmoovyog qhov dav-spectrum tshuaj tua kab uas muaj immunomodulatory. Its main functions include expelling intestinal parasites, regulating immune function, assisting in anti infection, assisting in anti-tumor treatment, and improving cellular immunity. Cov kev siv tshwj xeeb yuav tsum ua kom tau raws li tus kws kho mob cov kev taw qhia.
1. Ntiav Cov Kev Ploj Hlav
Levamisole inhibits cov kev ua si ntawm succinate hauv cab, cuam tshuam nrog cov hnyuv roj ntsha, thiab muaj kev sib tw ntawm cov roj av nematworms xws li cov kev sib tw ntawm cov roj av Cov tshuaj no muaj cov tshuaj pleev cov tshuaj zoo rau ob tus neeg laus thiab cov kab menyuam, tshwj xeeb yog tsim nyog rau kev kho kab mob kab mob.
2. Kev tswj hwm kev tiv thaiv kab mob
Cov tshuaj no tuaj yeem txhim kho cov lus teb rau mitogens, txhawb kev hloov pauv, thiab nce cov kev ua haujlwm ntawm kev ua yeeb yam ntawm macrophages thiab neurophils. Qhov kev tiv thaiv kab mob no ua rau nws haum rau kev kho cov kab mob uas cuam tshuam xws li kev ua pa kom rov qab ua pa thiab cov mob herpes.
3. Pab tiv thaiv kab mob anti kev tiv thaiv kab mob
Los ntawm kev txhim kho lub cev tiv thaiv kab mob ntawm lub cev, Levamisole tuaj yeem pab kev kho mob thiab kis tus kab mob.
Hauv kev siv tshuaj khomob regaileraly regimen rau mob ruas, feem ntau nws siv los ua ib qho kev hloov kho kom txhim kho kev kho mob.
4. Pab tiv thaiv kev tiv thaiv
Raws li tus neeg tiv thaiv kab mob tiv thaiv kab mob, cov tshuaj no tuaj yeem txhim kho cov tshuaj mob cancer rau kev sib xyaw ua ke ntawm cov qog ua ke xws li mob ntsws thiab mob ntsws. Nws tsis tau tawm tsam kev tawm tsam los ntawm cov qog ntshav los ntawm kev rov ua kom muaj kev tiv thaiv kev puas tsuaj.
5. Txhim Kho Cov Mob Cellular
Levamisole tuaj yeem xaiv rov qab kho dua t lymphocyte muaj nuj nqi thiab kho tsis muaj zog imbalance. Rau kev mob autoimmune xws li kev mob ntsws athumatoid erethematus, cov lus qhia tsis zoo, tab sis cov qauv qhia yuav tsum tau tswj hwm nruj.
Leamisole hmoov, raws li kev siv tshuaj hluavtaws nrog tshuaj kho kab ntsig thiab cov kev tswj hwm uas muaj zog, muaj cov tshuaj lom neeg ua haujlwm, siv tshuaj lom neeg, kev sib cais ob tog, thiab sib cais chiral. Kab lus no yuav rov xyuas cov txheej txheem tseem ceeb synthsis, los qhia cov tshuaj tiv thaiv kev ua haujlwm, ua ke nrog kev ua kom zoo dua qub, thiab kev hloov kho tau ntawm cov qauv sib txawv.
Txoj Kev 1: Tshuaj Siv Tshuaj Hluav Taws Xob: Txoj kev tseem ceeb ntawm kev lag luam
Cov tshuaj lom hluav taws xob synthsis txoj kev dominates dominates dominates dominates kev tsim cov leviisole vim nws cov tub ntxhais muaj txiaj ntsig zoo thiab tus me nyuam tsis tshua muaj zog los tsim kev tawm tsam ntau. Raws li qhov sib txawv hauv cov khoom pib, cov kev sib txuam tuaj yeem faib ua peb pawg: txoj kev acetophenone, cov qauv styrees, thiab epichlorohydrin.
1. Acetophenone Txoj Kev: Kev Txawj Ntse ntawm Cov Txheej Txheem Classic
Cov acetophenone txoj kev siv acetophenone raws li cov khoom siv pib los ntawm plaub kauj ruam: Halogenation, txo qis, thiab Cycloize
Acetophenone yog siv nrog bromine lossis chlorine los ua - bromoacetophenone. The reaction requires strict temperature control (0-5℃) to avoid multiple halogenated by-products. Piv txwv li, ib qho kev lag luam me sai sai ua cov tshuaj tiv thaiv kev ua kom luv luv ntawm cov tshuaj tiv thaiv lub sijhawm 6 teev rau 40 feeb, thiab cov txiaj ntsig nce rau 92%.
- Bromoacetophenone thiab 2-Aminothiazoline yauv ungogydrogenation nyob rau hauv Alkaline tej yam kev mob, ua rau tsim ntawm 2-imido-3-benzohlo-3-benzoylmethylthiazoline hydrohalide. Ib pab neeg tshawb fawb nce cov tshuaj tiv thaiv tawm los ntawm 75% los ntawm kev ntxiv theem hloov catalysts xws li tetrabutylamonium bromide.
Sodium borohydride lossis hydrogen yog siv los txo cov pab pawg ketone carbonyl, tsim kom muaj 2-im-im- (- hydroxyphenethyl) - Thiazoline. Ib qho kev lag luam muaj qee tus neeg ua haujlwm tau tsim cov palladium carbon catalytic hydrogenation txo ntawm 50℃thiab 3mpa, thiab 3mpa, thiab 3mpa, thiab 3mpa, thiab 3mpa, thiab 3mpa, thiab 3mpa, thiab 3mpa, thiab 3mpa, thiab 3mpaxyuas ntawm cov khoom qha ntawm 99.2%.
Lub cev qhuav dej thiab kev ua kom zoo nkauj hauv qab cov sulfuric acid matalysis tsim cov roj ntsha Lub thev naus laus zis tau ua rau lub sijhawm ua kom luv luv los ntawm 8 teev mus rau kev ua kom zoo dua cov roj sulfuric (85% -90%) thiab cov tshuaj tiv thaiv kub (110-120 degree).
Ib lub tuam txhab siv hluav taws xob loj tau saws cov txheej txheem acetophenone nrog ib xyoo ntau lawm muaj peev xwm ntawm 200 tons, thiab nws cov txheej txheem tseem ceeb muaj xws li:
Nruam halogenated cov tshuaj tiv thaiv cov khoom siv kom ua tiav kev pub mis ntawm bromine;
Membrane sib cais tshuab rov siv dua acetophenone, nce kev siv cov ntaub ntawv raw rau 98%;
Crystallization cov txheej txheem optimization, khoom passle loj faib d90 tsawg dua lossis sib npaug ntawm 50 μ m, sib tham txhaj cov kev txhaj tshuaj uas yuav tsum tau ua.
2. Styrene Txheej Txheem: Kev tshawb nrhiav kev hloov tshiab ntawm cov nyiaj siv
Cov txheej txheem styrene siv STYRENE yog cov khoom siv raw thiab tsim cov lus tseem ceeb ntawm peb kauj ruam ntxiv, kev sib txuas lus, thiab chlorination:
Ntxiv rau cov yeeb tshuaj tiv thaiv: styrene reacts nrog Dichhloroamine t nyob rau hauv Toluene los ua NP-Toluenesulforulforifre imine. Cov tshuaj tiv thaiv phot cov tshuaj tiv thaiv xav tau los tswj ntawm 8-9 kom tsis txhob imine hydrolysis.
Ntiv nplhaib kev tawm tsam: np-toluenesulforifeforifyres iMine yog condensed nrog aminoethanol thiab ces chlorinated nrog aminotsyled intermediat 3- (2-chloroethyl) -2-iminothiazolidine.
Kev Cuam Tshuam Cua: Raws li Alkaline cov xwm txheej, lub nplhaib raug kaw los ua daim ntawv
Technical bottleneck: Txoj kev no nthuav qhia cov kev cov nyom hauv qab no:
Tus nqi ntawm DICHHLOROAMINE T yog qhov tseem ceeb, kev suav nyiaj rau 40% ntawm tag nrho cov khoom siv raw tag nrho;
Cov tshuaj tua kab chlorination ua rau muaj ntau npaum li cas ntawm HCL roj, uas yuav tsum muaj kev txhawb nqa tus Tsov Zaum Roj Kho;
Cov qoob loo ntawm Chiral Cais kauj ruam tsuas yog 65%, ua rau muaj kev nce ntxiv hauv tag nrho cov nqi.
3. Epoxy Phenylethane txoj kev: kev coj ua hauv Green Chemistry
Lub Epoxyphenylethane txoj kev siv Epoxyphenyphenylethane raws li cov khoom siv raw thiab tsim cov qauv tseem ceeb ntawm ob kauj ruam qhib thiab kaw:
Ntiv qhib qhib cov tshuaj tiv thaiv: Epoxyphenyany thiab 2-chloroethyletinal thiab 2-chloroetide Foresliday Cov tshuaj tiv thaiv phot cov tshuaj tiv thaiv yuav tsum tau tswj hwm ntawm 9-10 kom tsis txhob amino oxidation.
Ntiv nplhaib kaw: MitsBobu cov tshuaj tiv thaiv yog siv los ua tiav intramolecular lub nplhaib kaw thiab tsim Levamisole hauv paus. Qhov tshuaj tiv thaiv no tau siv tripherylphs thiab Azodicarboxylate Dioter (tuag) raws li reagents, uas muaj qhov zoo ntawm kev ua siab zoo thiab cov tshuaj tiv thaiv me me.
Industrial kev nce qib: ib qho kev nce qib tau tsim cov Flow txaus MitsTunobu cov khoom siv, ua tiav cov kev sib tawg hauv qab no:
Lub sijhawm kev tawm tsam tau raug luv los ntawm cov kaus mom tsoos Kettle 0 teev rau 2 teev;
Txo cov nyiaj reagents los ntawm 50%, thiab rov ua dua tus nqi ntawm tripyenyypphephphine nce mus txog 90%;
Lub ce kho qhov muag ntawm cov khoom mus txog 99.5%, ntsib cov qauv ntawm European Pharpacopoeia.
Txoj Kev 2: Kev Tshawb Fawb Txog Kev Tshawb Fawb: Kev tshawb nrhiav ntawm cov thev naus laus zis ib puag ncig
Biosynthetic txoj kev siv enzyme catalysis los yog microbial kev hloov pauv kom ua tiav kev tsim ntsuabLeamisole hmoov, nrog nws cov ntsiab lus tseem ceeb yog cov tshuaj tiv thaiv me me thiab kev xaiv siab.
1. Enzyme catalyzed synthesis: kev kho kom zoo ntawm chairal chaw
Ib pab pawg tshawb fawb siv transaminase catalyzed asymmetric syntheis ntawm acetophenone derivatives:
Substrate tsim: synthesize acetophenone-2-amine raws li enzyme catalyzed substrate, thiab kev ncua deb ntawm nws amino thiab carbonyL pab cuam tshuam rau cov kev khi ntawm enzyme chaw.
Enzyme Ntsuam Xyuas: L-Spiration Transaminase tau soj ntsuam los ntawm av cov microorganisms, nrog rau tus nqi km ntawm 0.5 s ⁻¹.
Cov tshuaj tiv thaiv optimization: raws li PH 7.5 thiab 37℃cov kev mob, tus nqi piv txwv li cov khoom hu rau 99% tom qab 24 teev ntawm cov tshuaj tiv thaiv.
Kev sib ntaus sib hauj lwm cov nyom:
Tus nqi enzyme npaj yog tus kheej kuj tseem ceeb, cov nyiaj txiag rau 35% ntawm cov nqi tsim khoom;
Tsawg substrate solubility yuav tsum tau tsim kho cov kuab tsav tshiab;
Kev sib cais ntawm cov khoom lag luam xav tau kev siv simulated txav lub txaj chromatography, uas yuav tsum muaj peev xwm loj tshaj.
2. Microbial kev hloov pauv: tshawb nrhiav lub peev xwm ntawm tag nrho cov xovtooj ntawm tes
Lub tshuab ua haujlwm ua thev naus laus zis ntawm cov paxeeb astilizes sp. Tag nrho cov xovtooj ntawm tes ua rau letraamisole los ntawm acetophenone:
Kev hloov kho tshiab: los ntawm kev txhim kho lub dehalogenase thiab kev ua ub no ntawm kev sib cav los ntawm cov gene editing, qhov kev hloov dua siab tshiab tau nce ntxiv ntawm 15% mus rau 68%.
Fermenation optimization: tau txais cov batch Pub feeding lub tswv yim, 0.5% acetophenone tau ntxiv nyob rau 24 teev cov khoom lag luam ntawm 4.2 g / l.
Kev sib cais: Siv macroporption cov qauv, qhov kev coj dawb huv ntawm cov khoom lag luam ncav tau txog 98% thiab tus nqi rov qab yog 85%.
Kev Ntsuam Xyuas Nyiaj Txiag:
Tus nqi ntawm cov khoom siv raw yog txo los ntawm 20% piv rau txoj kev siv tshuaj;
Lub voj voog fermentation siv sijhawm li 72 teev thiab cov khoom siv hloov pauv qis;
Tus lej cod ntawm cov dej lwg yog txo los ntawm 60% piv rau cov qauv siv tshuaj, uas muaj cov kev zoo ib puag ncig.
Kev Loj Hlob:
Kev Tsim Nruag:
Cov thev naus laus zis xws li Microchannel Reactors thiab Nruam Nruam Crystallization yuav txhawb nqa cov tshuaj lom neeg syntheis rau kev ua haujlwm siab thiab kev nyab xeeb.
Kev Raug Mob Biological:
Synthetic biology siv tau kom ua tiav kev npaj qis ntawm enzyme npaj, tawg los ntawm kev lag luam botteneck ntawm biosyntheis.
Green Chemistry:
Hnyav rov qab, atomic kev txhim kho kom zoo thiab lwm txoj kev yuav txo qis kev tsim kho cov khoom muaj.
Synthei technology ntawmLeamisole hmoovtab tom hloov pauv kev hloov pauv ntawm cov tshuaj lom neeg rau cov kev sib txuas lus ntsuab thiab kev tsim khoom txuas ntxiv. Nyob rau hauv lub neej yav tom ntej, nrog kev tawg hauv ai pab enzyme tsim, txuas ntxiv cov txheej txheem, thiab lwm yam kev sib sau ua ke, tus nqi qis, thiab kev ua tau zoo dua qub.
Cim npe nrov: Levamisole hmoov, lwm tus neeg, chaw tsim khoom, Hoobkas, lag luam wholesale, yuav, nqe, loj, loj, rau muag