N - boc - l - prolinal, tseem hu ua boc - l -} poline} polbroffrolidine-1-carboxylic acid tert butter, yog qhov sib xyaw. Nyob rau hauv chav tsev kub thiab siab, nws yog lub teeb pom kev zoo lub teeb xim daj uas muaj qhov sib txheeb nrog kev txheeb ze ntawm 1.148 g / cm3. Nyuaj kom yaj hauv dej, tab sis soluble nyob rau hauv cov organic cov kuab tshuaj thiab muaj cov tshuaj tua kab mob siab thiab muaj cov tshuaj tua kab mob. Cov pab pawg BOC tuaj yeem tshem tawm tau yooj yim, thiab aldehyde pab pawg yuav hloov mus rau pawg hydroxyl los ntawm kev txo lossis pab pawg cyanide los ntawm cyanide cov tshuaj tiv thaiv. Nws yog feem ntau siv rau kev tshawb fawb thiab kev siv cov ntawv thov.
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Tshuaj Cov Qauv |
C10H17No3 |
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Muaj pes tsawg leej |
199.12 |
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Molecular hnyav |
199.25 |
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m/z |
199.12 (100.0%), 200.12 (10.8%) |
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Kev Ntsuam Xyuas |
C, 60.28; H, 8.60; N, 7.03; O, 24.09 |
Nws ua lub luag haujlwm tseem ceeb nyob rau hauv cov synthesis ntawm amino haus dej haus thiab cov tshuaj hormones roj ntsha. Nws cov qauv tshuaj tshwj xeeb pub rau qhov kev sib koom tes rau hauv cov qauv molecules, yog li pab txhawb cov hluavtaws ntawm cov kev ua haujlwm biological no.
N - boc - l - prolinalRaws li nrab nruab nrab nyob rau hauv synthesis ntawm amide -}}}}}}}}}} part hiv tus neeg inhibitors, nws ua rau muaj kev txhim kho cov tshuaj antiretroviral. Nws teeb tsa mus rau hauv cov kev sib tw ua ke tau muab lub tsev loj heev rau kev tsim cov Hiv tus neeg phem.
Cov pab pawg BOC hauv nws muab cov teeb meem hauv cov tshuaj lom hluav taws xob. Cov pab pawg no tuaj yeem siv tau yooj yim, tso cai rau kev ua haujlwm ntxiv thiab cov qauv hloov kho ntawm cov molecule. Cov yam ntxwv no txhim kho cov versatility hauv cov versatility hauv kev tshawb tshuaj yeeb thiab tshuaj synthesis.
Cov pab pawg aldehyde hauv nws tuaj yeem ua rau muaj kev hloov pauv ntau ntxiv. Piv txwv li, nws tuaj yeem raug txo mus rau cov pab pawg hydroxyl lossis hloov mus rau hauv ib pab pawg Cyano los ntawm kev txo qis thiab Cyalation. Cov kev hloov pauv no nthuav dav cov khoom siv hluavtaws thiab pab cov hluavtaws ntawm ntau yam kev lom neeg tshuaj lom neeg.
5.YSyim ntawm Bioactive Peptide Meptetics
Nws yog ib qho kev nthuav dav proline uas muaj cov bom tiv thaiv pab pawg, xws li Dolastatin 10 analogs nrog Antiols Cancer tej kev ua si.
6.Cov tshuaj tiv thaiv vinylation
Nws tuaj yeem ua lub tsev tseem ceeb hauv kev sib txuas ntawm cov hluav taws xob muaj cov amino acid qauv. Tsis tas li ntawd, nws nucleophilic ntxiv cov kev pom zoo thiab cov tshuaj tiv thaiv alkynylation tuaj yeem siv los synlex cov qauv ntawm cov lus sib txuas, nthuav tawm cov kev tawm tsam organic.
7. Muaj cov ntawv thov
Vim nws cov versatility thiab qhov tseem ceeb hauv cov tshuaj synthesis, nws yog dav siv hauv kev siv cov ntawv thov. Nws ua haujlwm rau qhov tseem ceeb hauv kev tsim khoom ntawm cov tshuaj ntawm cov tshuaj, cov khoom lag luam biochemicals, thiab lwm yam khoom lag luam uas cuam tshuam.
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Qhov Tseem Ceeb hauv Hiv Inhooritor Tshawb Nrhiav
1.Qhov kev cuam tshuam ntawm kev kho mob
(1.) Muab cov kev kho mob tshiab: Hiv Inhibitors muab cov neeg kho mob tshiab rau HIV cov tshuaj tiv thaiv HIV, tshwj xeeb rau cov neeg uas tsim tawm cov tshuaj tiv thaiv kab mob los yog muaj kev xav tau tshwj xeeb.
(2.) Txhim kho kev txhim kho kev ua tau zoo: Qee cov kabmob HIV, thaiv tus kab mob replication thiab muab tus kab mob pib ntawm tus kab mob HIV. Cov tshuaj no tau pom cov kev cuam tshuam tseem ceeb hauv kev sim tshuaj thiab yuav tsum txhim kho kev ua tiav HIV.
(3.) Txo cov kev phiv tshuaj tawm: cov tshuaj antiretroveiral (kos duab) yuav xav tau kev tswj hwm nquag thiab yuav nrog qee qhov kev mob tshwm sim. Ntev ua rau HIV inhibitors, xws li Lenbapitir, uas tsuas yog yuav tsum tau muab ob zaug ib xyoos, tuaj yeem txo cov tshuaj muaj tsawg zaus thiab cov kev mob tshwm sim, thiab txhim kho lawv lub neej zoo.
2. Kev tiv thaiv kev tiv thaiv kab mob HIV
(1.) Ua ntej tshaj tawm Prophylaxis (Prep): Qee qhov kev tiv thaiv kab mob HIV, tsis txhob muaj kab mob nrog tus kab mob liab (Shiv). Cov tshuaj no yuav tsum tau siv rau ua ntej raug cov yaj saub tau los ntawm tib neeg, txo qhov kev pheej hmoo ntawm tus kabmob HIV.
(2.) Txo cov kab mob kis: los ntawm kev hloov pauv tus kabmob HIV, yog tsis muaj kev pheej hmoo ntawm cov kab mob kis rau lwm tus neeg los ntawm kev sib daj sib deev, thiab lwm txoj kev.
3.Cromote qhov kev kawm ntawm kev tshawb nrhiav HIV
(1.) Txhawb txoj kev txhim kho cov tshuaj tshiab: Kev tshawb fawb thiab kev txhim kho cov Hiv Inhibitors tau ua rau cov kws tshawb fawb kev tshawb fawb thiab cov tswv yim ntxiv.
(2.) Hauv kev nkag siab tob ntawm HIV
4.imvact ntawm cov zej zog thiab kev lag luam
(1.) Kev kho mob lub nra: kev loj hlob thiab kev siv ntawm tus kab mob HIV tuaj yeem pab txo cov nqi kho mob thiab txhim kho kev ua haujlwm ntawm cov neeg mob kho mob.
(2.) Kev txhim kho cov neeg mob lub neej: Los ntawm kev txo cov tshuaj cuam tshuam thiab kev txhim kho kev ua kom mob siab rau cov neeg mob lub neej thiab kev koom tes hauv zej zog, txo lub nra rau hauv zej zog thiab tsev neeg.
Cov hau hluav taws xob
Cov Qauv Swev Oxidation:
- Reagents thiab cov xwm txheej: Siv Oxalyl chloride, DMOPS, thiab Triethylamine hauv -78℃cov xwm txheej.
- Kev ua: N {- boc {{1} l}}}}}}}}}}}}}}}}}}}}}}}} l} Txawm li cas los xij, cov qauv no yuav tsum muaj tej yam kev mob tsis muaj kev kub ntxhov thiab kub tsawg, ua rau nws nyuaj rau kev siv cov ntawv thov kev lag luam.
DMOPS oxidation nrog li3-pyridine complex:
- Tshuaj tivthaiv: DMOPS raws li oxidant, khoom li3-pyridine complex raws li tus activator, thiab Triethylamine raws li lub hauv paus.
- Kev ua: N {- boc- l}}}}}}}}}}} {-pyridine complex, thiab triethylamine. Txoj kev no tseem ua rau muaj kev tsis zoo ntawm Sadethyl sulfide.
Dess - martin oxidation:
- Reagent: Siv cov Dess - Martin Timominane (DMP) oxidant.
- Kev ua: N {{- boc {1} l {{{2} - Martin perpininane reugent. Thaum cov qauv no ua tau zoo, lub reagent nws tus kheej yog tus kheej, txwv nws tus nqi {{5 6}} nplai synthesis.
Lub ntsiab:
- Qhov kev xaiv ntawm cov qauv hluav taws xob rau nws nyob ntawm qhov tshwj xeeb ntawm cov kev xav tau ntawm synthesis, xws li muaj kev tiv thaiv ntawm cov khoom lag luam, kev txiav txim siab tau txais txiaj ntsig zoo ntawm cov khoom.
- Cov txheej txheem swern oxidation, thaum ua haujlwm nyuaj, yog qhov nyuaj vim tias yuav tsum tau muaj qee qhov kev mob thiab kub tsawg.
- Txoj kev DMOPS oxidation, thaum yooj yim, ua rau tsis muaj ntxhiab tsw.
- Cov Dess - martin oxidation txoj kev ua haujlwm zoo tab sis kim.
Keeb kwm yav dhau los ntawm kev tshawb pom
N - boc - l - prolinal, lub ntsiab lus organic hluavtaws nruab nrab, pom nws qhov tseem ceeb hauv kev ntsuas tshuaj thiab asymmetric matalysis. Nws qhov kev tshawb pom thiab cov ntawv thov txuas ntxiv yog cov hauv paus hauv kev nkag siab thiab siv cov tshuaj lom neeg, uas muaj cov tshuaj lom thiab ua haujlwm.
- {{0} Amino aldehydes muaj ib pawg tshwj xeeb ntawm cov pab pawg ua ke thiab kev tiv thaiv amino. Cov kev teeb tsa no cov qauv uas tau txais txiaj ntsig lawv muaj txiaj ntsig zoo, ua rau lawv muaj txiaj ntsig zoo ntawm cov khoom siv hauv siab.
- Lawv tuaj yeem muab tau los ntawm - cov amino acids, los ntawm kev hloov pauv ntawm - kua roj ntawm cov amino cawv.
- Tshwj xeeb, yog ib qho tseem ceeb organic hluavtaws nruab nrab vim nws lub luag haujlwm hauv cov synthesis ntawm ntau txoj kev muaj xyoob ntoo. Piv txwv li, nws ua haujlwm ua tus tseem ceeb hauv nruab nrab hauv cov synthesis ntawm hiav txwv hare toxin.
- Nws boc (tert - butoxycarbonyl) pab pawg muaj kev tiv thaiv kev tiv thaiv rau cov tshuaj amino, tso cai rau kev kho cov tshuaj ntxiv thaum khaws cov amino ua haujlwm.
- Kev tshawb nrhiav thiab nws cov hluavtaws hluav taws xob tau tsav los ntawm kev xav tau ntawm txoj kev ua kom zoo rau synthesize muaj kev sib txuas ua ke. Raws li qhov tshwm sim, ntau txoj hauv kev tau tsim los ua hluavtaws cov nruab nrab no los ntawm - cov amino acids lossis lawv cov acids lossis lawv cov derivatives.
- Nws cov ntawv thov Spell los ntawm cov khoom siv tshuaj yeeb, qhov twg nws pab ua ke nruab nrab ntawm Hiv Inhomitors thiab lwm yam BioymTric cathevy, uas siv tau los ua cov chiral liigand lossis catalyst.
Kev lag luam loj txuas ntxiv mus nthuav dav
Nrog rau kev txhim kho sai ntawm kev lag luam thoob ntiaj teb xws li tshuaj thiab tshuaj thiab kev nce ua lag luam txuas ntxiv hauv khw xav tau, nws yuav txuas ntxiv mus ntxiv. Tshwj xeeb tshaj yog nyob rau hauv kev tshawb fawb, kev tsim kho thiab kev tsim cov tshuaj rau cov kab mob loj xws li mob qog noj ntshav xws li maj nrawm. Lub caij no, nrog rau sawv ntawm cov teb chaws tawm hauv khw thiab kev txhim kho ntawm cov neeg siv kev noj qab haus huv, kev thov lag luam hauv Tebchaws Asia thiab Africa yuav nce ntxiv.
Thev naus laus zis ua luam tawm
Kev siv thev naus laus zis yog qhov kev tsav tsheb tseem ceeb rau kev txhawb nqa kev lag luam. Yav tom ntej, nrog kev nce qib nruam ntawm cov khoom siv hluavtaws organic thiab kev siv cov tshuaj tiv thaiv kab mob tshiab, nws cov khoom siv hluav taws xob yuav ua kom tau zoo txuas ntxiv thiab hloov kho tshiab. Qhov no yuav pab ua kom muaj kev vam meej txhim kho ntau lawm, txo cov nqi tsim khoom, txhim kho cov khoom siv purity thiab zoo ruaj khov. Nyob rau tib lub sijhawm, thev naus laus zis yuav tseem yuav txhawb nqa cov kev nthuav dav ntawm cov ntawv thiab kev siv cov kev tsim kho hauv ntau daim teb.
Kev tiv thaiv ib puag ncig cov cai muaj kev txhim kho ntsuab ntxiv txhawb kev loj hlob ntxiv
Nrog rau kev nce thoob ntiaj teb ntawm kev tiv thaiv ib puag ncig thiab cov kev cai nruj zuj zus, kev lag luam ntau lawm yuav ntsib ntau lub sijhawm ib puag ncig. Txawm li cas los xij, qhov no tseem yuav txhawb cov neeg lag luam kom ntxiv dag zog rau cov kev tshawb fawb thiab kev txhawb nqa kev tiv thaiv kev tiv thaiv kev lag luam, thiab txhawb txoj kev loj hlob ntawm kev lag luam. Nyob rau hauv lub neej yav tom ntej, kev lag luam ntau lawm yuav them ntau dua rau kev tiv thaiv hluav taws xob, kev tiv thaiv ib puag ncig, kev siv hluav taws xob ua tiav, kev siv nyiaj los yog kev lag luam ib puag ncig kev lag luam thiab cov txiaj ntsig.
Ntxiv dag zog rau kev koom tes thoob ntiaj teb thiab sib pauv
Nrog qhov tob ntawm kev lag luam thoob ntiaj teb thiab kev nce ntau ntawm kev ua lag luam thoob ntiaj teb, koom tes thoob ntiaj teb thiab kev sib pauv hauv kev lag luam no yuav txuas ntxiv ntxiv dag zog. Qhov no yuav pab cov tuam txhab ua kom muaj kev kawm zoo hauv kev nkag siab thoob ntiaj teb kev thov kev lag luam thiab kev paub txog kev lag luam tshaj lij, thiab kev nthuav dav ua lag luam, thiab nthuav dav kev lag luam txawv teb chaws. Nyob rau tib lub sijhawm, kev koom tes thoob ntiaj teb thiab kev sib pauv tseem yuav txhawb txoj kev txhim kho kev lag luam tshiab thiab ua kom nrawm nrawm ntawm kev siv txhim kho.
Cim npe nrov: n - boc - l {polon-}}}, cov chaw tsim khoom, chaw muag khoom, yuav khoom, loj, rau muag