1H-Isoindol -3-amine Hydrochloride CAS 76644-74-1

Synthetic Routes thiab Reaction Conditions:Kev sib xyaw ntawm 3-Amino-1H-isoindole hydrochloride feem ntau cuam tshuam nrog cov tshuaj tiv thaiv ntawm 1H-2,4-benzodiazepine nrog methoxy pawg hauv cov xwm txheej tshwj xeeb. Cov txheej txheem suav nrog cov kauj ruam xws li amination siv hypervalent iodine reagents thiab Larock annulation . Cov tshuaj tiv thaiv kab mob feem ntau xav tau qhov ntsuas kub thiab siv cov catalysts tshwj xeeb kom ntseeg tau tias cov khoom xav tau.

Kev Tsim Kho Kev Lag Luam:Hauv cov chaw tsim khoom, kev tsim cov khoom sib xyaw no tuaj yeem koom nrog kev sib xyaw ua ke loj uas siv cov tshuaj tiv thaiv zoo tshaj plaws los ua kom muaj txiaj ntsig zoo tshaj plaws thiab purity. Cov txheej txheem yog tsim los ua kom muaj txiaj ntsig zoo thiab muaj txiaj ntsig zoo, feem ntau suav nrog cov txheej txheem siab heev xws li kev sib txuas txuas txuas ntxiv thiab kev soj ntsuam cov tshuaj tiv thaiv automated.

Heterocyclic chemistry yog ib qho tseem ceeb tshaj plaws ntawm cov khoom siv tshiab nrog ntau hom kev ua haujlwm lom neeg, feem ntau vim yog lub peev xwm tshwj xeeb ntawm cov khoom sib xyaw ua ke los ua cov qauv ntawm peptides thiab khi reversibly rau cov proteins. Rau cov kws kho mob tshuaj, qhov txiaj ntsig tseeb ntawm cov qauv heterocyclic yog lub peev xwm los tsim ib lub tsev qiv ntawv raws li ib qho tseem ceeb scaffold thiab los tshuaj xyuas nws tawm tsam ntau yam sib txawv receptors, yielding ob peb active compounds. Yuav luag tsis muaj kev txwv kev sib txuas ntawm fused heterocyclic cov qauv tuaj yeem tsim tau, ua rau cov qauv tshiab polycyclic nrog ntau lub cev, tshuaj lom neeg thiab cov khoom siv lom neeg. Lub fusion ntawm ob peb lub nplhaib ua rau geometrically zoo-txhais nruj cov qauv polycyclic thiab, yog li, tuav cov lus cog tseg ntawm kev ua haujlwm siab tshwj xeeb uas tshwm sim los ntawm kev muaj peev xwm rau orient hloov pauv hauv peb qhov chaw. Yog li ntawd, cov txheej txheem ua tau zoo uas ua rau muaj cov qauv polycyclic los ntawm cov qauv siv tshuaj lom neeg heterocyclic ib txwm muaj kev txaus siab rau ob qho tib si organic thiab tshuaj chemists.

Cov khoom sib xyaw nrog heterocyclic rings yog inextricably woven rau hauv cov txheej txheem biochemical ntawm lub neej. Yog hais tias ib tug yuav tsum xaiv ib kauj ruam nyob rau hauv ib tug biochemical txoj kev ntawm random yuav muaj ib tug zoo heev lub sij hawm uas ib tug ntawm cov reactants los yog cov khoom yuav yog ib tug heterocyclic compound. Txawm hais tias qhov no tsis muaj tseeb, kev koom tes ntawm heterocycles hauv cov lus nug hauv cov lus nug yuav luag txhua qhov kev hloov pauv biochemical yog catalyzed los ntawm enzymes, thiab peb ntawm nees nkaum amino acids pom nyob rau hauv enzymes muaj heterocyclic rings. Ntawm cov no, lub nplhaib imidazole ntawm histidine tshwj xeeb yuav muaj feem cuam tshuam; histidine muaj nyob rau ntawm qhov chaw nquag ntawm ntau cov enzymes thiab feem ntau ua haujlwm raws li cov kua qaub-puag lossis ua hlau ion ligand. Tsis tas li ntawd, ntau cov enzymes ua haujlwm tsuas yog muaj qee qhov me me uas tsis yog-amino acid molecules hu ua coenzymes (los yog cofactor), uas feem ntau tsis yog heterocyclic compounds. Tab sis txawm hais tias cov enzyme hauv nqe lus nug tsis muaj ib qho ntawm cov coenzymes lossis peb cov amino acids uas tau hais los saum toj no, lub luag haujlwm tseem ceeb tseem yuav raug ntaus los ntawm heterocycles vim tias tag nrho cov enzymes raug tsim los ntawm txoj cai hauv DNA, uas tau piav qhia los ntawm cov kab ke. ntawm heterocyclic bases pom nyob rau hauv DNA.

Tshuaj kho mob muaj kev txhawj xeeb txog kev kho cov kab mob sib kis, kab mob cab lossis kab mob malignant los ntawm cov tshuaj siv tshuaj, feem ntau yog cov tshuaj uas qhia txog kev xaiv toxicity rau cov kab mob. Cov kab mob ntawm lub cev tsis ua haujlwm thiab cov neeg ua haujlwm ua haujlwm feem ntau yog cov sib txuas uas cuam tshuam rau kev ua haujlwm ntawm cov enzymes, kev xa cov paj hlwb lossis kev ua haujlwm ntawm cov tshuaj hormones ntawm receptors. Heterocyclic tebchaw yog siv rau tag nrho cov hom phiaj no vim hais tias lawv muaj ib tug tshwj xeeb tshuaj reactivity piv txwv li epoxides, aziridines thiab -lactams, vim hais tias lawv zoo li cov metabolites tseem ceeb thiab muaj peev xwm muab tsis tseeb synthons nyob rau hauv biosynthetic dab, piv txwv li antimetabolites siv nyob rau hauv kev kho mob cancer thiab kab mob. vim tias lawv haum rau cov receptors lom thiab thaiv lawv cov kev ua haujlwm ib txwm muaj, lossis vim tias lawv muab cov khoom siv yooj yim rau cov khoom siv roj ntsha. hloov pauv tuaj yeem txuas nrog. Kev qhia txog cov pab pawg heterocyclic rau hauv cov tshuaj yuav cuam tshuam rau lawv lub cev, piv txwv li kev sib cais ntawm cov tshuaj sulfa, lossis hloov lawv cov qauv ntawm kev nqus, metabolism lossis toxicity.

Ntau qhov kev tshawb pom tseem ceeb tau ua, txawm li cas los xij, los ntawm kev txhim kho kev soj ntsuam ntawm kev ua haujlwm lom neeg ua los ntawm kev ua haujlwm tsim los rau lwm qhov kawg, lossis thaum lub sijhawm siv tshuaj kho mob qhia rau lwm lub hom phiaj. Lub hauv paus theoretical ntawm cov tshuaj chemistry tau dhau los ua ntau yam tshiab, tab sis yog qhov tsis zoo xav tias qhov kev tshawb pom ntawm cov tshuaj tsuas yog ib qho teeb meem ntawm kev sib raug zoo ntawm kev ua haujlwm. Kev vam meej ntawm tus neeg sawv cev tshuaj yog nyob ntawm qhov sib npaug ntawm nws cov txiaj ntsig pharmacological thiab qhov kev puas tsuaj uas nws yuav ua rau tus neeg mob, thiab qhov no tseem tsis tuaj yeem ua rau muaj tseeb. Serendipity thiab hmoov zoo yuav tsis ua xyem xyav mus ua ib feem tseem ceeb hauv kev tshawb pom tshiab.

Indole alkaloids yog bicyclic compounds uas muaj rau lub nplhaib benzene fused rau tsib lub nplhaib pyrrole. Vim muaj cov nitrogen atom nyob rau hauv lub nplhaib pyrrole, indole alkaloids muaj cov yam ntxwv tseem ceeb uas ua rau lawv cov tshuaj siv tshuaj. Indole alkaloids tuaj yeem pom muaj nyob hauv ntau tsev neeg cog, suav nrog Loganiaceae, Apocynaceae, Nyssaceae, thiab Rubiaceae. Loj indole alkaloids cais los ntawm cov nroj tsuag muaj xws li active molecules uas muaj zog tiv thaiv kab mob ntsws, xws li vincristine, vinblastine, thiab lwm yam, thiab vincristine yog ib qho tseem ceeb tshaj plaws indole alkaloidal tebchaw, uas tag nrho cov muaj peev xwm pab tau rau kev kho mob ntawm cov neeg mob pulmonary kab mob, xws li tuberculosis, hawb pob, emphysema, pulmonary fibrosis, thiab mob qog noj ntshav.

Txawm li cas los xij, qee qhov ntawm cov tebchaw no tau pom tias muaj kev phom sij rau lub cev. Tsis tas li ntawd, ib qho kev tswj hwm ntawm alkaloids cais los ntawm Alstonia scholaris cuam tshuam rau nas tus cwj pwm ntawm koob tshuaj ntawm 12.8 g / kg lub cev qhov hnyav (BW) thaum noj nyob rau hauv ib qho chaw, uas ua rau hawb pob, ua tsis taus pa, thiab convulsions hauv nas. Vinblastine, muab tau los ntawm Catharanthus roseus, yog ib qho vinca alkaloid nrog antineoplastic kev ua haujlwm uas tau ua rau muaj kev cuam tshuam tsis zoo rau lub cev, xws li kev tsis haum tshuaj hnyav, los ntshav hnyav, mob pob txha toxicity, o, mob pob txha, ntshav hauv zis, cem quav, mob taub hau. , ntuav, mob plab, mob ua pa luv, tsis qab los noj mov, thiab sib sib zog nqus kab mob. Qee qhov sib xyaw ua ke tau raug sim hauv tsev kho mob kom paub tseeb qhov kev kho mob tau tsim nyob rau hauv vitro thiab hauv vivo kev sim.

Alkaloids yog cov metabolites thib ob tseem ceeb tshaj plaws thiab tau siv rau ntau tshaj 4000 xyoo thiab vim lawv txoj kev kho mob loj heev (Amirkia thiab Heinrich, 2014). Xyoo 1818, alkaloids tau piav qhia thawj zaug los ntawm.

Meissner, uas siv lo lus los piav txog tag nrho cov organic molecules muab los ntawm cov nroj tsuag uas tuaj yeem paub qhov txawv raws li qhia cov yam ntxwv (Preininger, 1975). Alkaloids tuaj yeem muab faib ua ntau pawg nyob ntawm lawv cov qauv, suav nrog indoles, quinolines, isoquinolines, pyridines, pyrrolidines, pyrrolizidines, tropanes, steroids, thiab terpenoids. Ntawm cov ntau hom alkaloids no, indole alkaloids sawv cev rau kev sib sau ua ke ntawm nitrogen-muaj cov molecules thiab ntau yam ntawm chav kawm ntawm alkaloid no muaj nyob. Vim muaj ntau yam ntau yam uas tau txheeb pom, ntau pab pawg tom qab tau sib txawv, suav nrog yohimbans (reserpine, yohimbine, thiab deserpidine), strychnos alkaloids (strychnine, brucine, thiab vomicine), heteroyohimbans (ajmalicine), reserpines (aserpines). vinblastine, vincristine, thiab vinflunine), kratom alkaloids (mitragynine), ergolines/clavinet alkaloids (ergine, ergotamine, thiab lysergic acid), beta-carbolines (harmine thiab harmaline), tryptamines (psilocybin thiab serotonin), thiab Tabernanthe iboga alkonaaloids (iboga alkonaaloids), voacangine). Cov indole alkaloids no tuaj yeem pom nyob rau hauv hom los ntawm ntau tshaj 30 tsev neeg botanical, xws li Apocynaceae, Passifloraceae, Loganiaceae, thiab Rubiaceae, ntxiv rau cov fungi.