Baloxavir Marboxil CAS 1985606-14-1 API Factory High Quality
I-Shanghai Ruifu Chemical Co., Ltd. ngumenzi ohamba phambili we-Baloxavir Marboxil (CAS: 1985606-14-1) enomgangatho ophezulu.I-Ruifu Chemical inokubonelela ngenkonzo yehlabathi jikelele, ixabiso elikhuphisanayo, inkonzo egqwesileyo, encinci kunye nezixa ezininzi ezikhoyo.Thenga iBaloxavir Marboxil,Please contact: alvin@ruifuchem.com
Igama leMchiza | Baloxavir Marboxil |
Izithethantonye | BXM;S-033188 |
Inombolo yeCAS | 1985606-14-1 |
Ubume beStokhwe | Kwi-Stock, iMveliso yeMveliso ukuya kumakhulu eeKilogram |
Ifomula yeemolekyuli | I-C27H23F2N3O7S |
Ubunzima beMolekyuli | 571.55 |
Ukuxinana | 1.57±0.10 g/cm3 |
Ukunyibilika | Inyibilika kwi-DMSO |
Ugcino Lwexesha elide | Gcina Ixesha elide kwi -20 ℃ |
I-COA kunye ne-MSDS | Iyafumaneka |
Imvelaphi | Shanghai, China |
Uphawu | Ruifu Chemical |
Into | Iinkcukacha |
Imbonakalo | Mhlophe ukuya kwi-Off-White Powder |
Ukuchongwa | I-IR Spectrum ihambelana nomgangatho wereferensi Ixesha lokugcinwa lihambelana nomgangatho wereferensi |
Isiqulatho samanzi (nge-KF) | ≤1.0% |
Ilahleko ekomisweni | ≤1.0% |
Intsalela kwi-Ignition | ≤0.50% |
Iintsimbi ezinzima | ≤20ppm |
Izinto ezinxulumeneyo | |
Ubuninzi bokungcola komntu ngamnye | ≤0.50% |
Ukungcola ngokupheleleyo | ≤1.0% |
Ubungakanani beNcam | D90 Dlula 150um |
Ucoceko lweChiral | ≥99.0% |
Ubunyulu | ≥99.0% |
Isivavanyi | 98.0%~102.0% |
Izinyibilikisi ezishiyekileyo | Thobela iiMfuno zeICH |
Ukuhambisa ngenqanawe | Ukuthumela ngePakethi yomkhenkce |
Umgangatho woVavanyo | Umgangatho woShishino |
Ukusetyenziswa | I-API, kunyango lwe-Influenza A kunye ne-Influenza B Infections |
Umqulu:Ibhotile, ingxowa yefoyile yeAluminiyam, 25kg/Igubu lekhadibhodi, okanye ngokwemfuno yomthengi.
Imeko yoGcino:Gcina isikhongozeli sivalwe ngokuqinileyo kwaye usigcine kwindawo epholileyo, eyomileyo (2~8℃) kunye nendawo yokugcina impahla engena moya ikude kwizinto ezingahambelaniyo.Khusela ukukhanya kunye nokufuma.
Ukuhambisa ngenqanawe:Zisa kwihlabathi liphela ngomoya, ngeFedEx / DHL Express.Ukubonelela ngokukhawuleza nangokuthembekileyo.
I-Baloxavir Marboxil (i-CAS: 1985606-14-1, BXM, S-033188, Xofluza) lichiza le-antiviral elaphuhliswa nguShionogi Co., inkampani yaseJapan yamachiza kunye neRoche kunyango lwe-influenza A kunye ne-influenza B yosulelo.Ichiza lavunywa ekuqaleni ukuba lisetyenziswe eJapan ngoFebruwari 2018 kwaye lamkelwa yi-FDA ngo-Okthobha wama-24, 2018 kunyango lomkhuhlane onzima onzima kwizigulana ezineminyaka eyi-12 ubudala nangaphezulu eziye zabonakalisa iimpawu ezingekho ngaphezu kweeyure ezingama-48.I-Baloxavir marboxil, i-cap-endonuclease inhibitor, inendlela eyodwa yokusebenza xa ithelekiswa nodidi lwangoku lwe-neuraminidase inhibitor inhibitor esetyenziselwa ukunyanga usulelo lomkhuhlane.I-Baloxavir Marboxil lichiza elitsha lokulwa umkhuhlane elinendlela entsha yokusebenza.I-Baloxavir Marboxil liyeza le-Baloxavir Acid (S-033447) elinqanda ngamandla nangokukhetha i-cap-dependent endonuclease ngaphakathi kwe-polymerase PA subunit yomkhuhlane wentsholongwane A kunye no-B, ekhokelela ekuthinteleni ushicilelo nophindaphindo lwe-RNA.I-Baloxavir iphandwe ukuba inganakho ukunyanga i-COVID-19 kodwa akukho ncedo luqinisekisiweyo lubonakalisiweyo.
I-Baloxavir Marboxil yiarhente yonyango lomkhuhlane, ngokukodwa, inhibitor ye-enzyme ejolise kwi-cap-dependent endonuclease yentsholongwane yomkhuhlane, omnye wemisebenzi yentsholongwane yepolymerase complex.Ngokukodwa, inqanda inkqubo eyaziwa ngokuba yi-cap snatching, apho intsholongwane ifumana i-primers emfutshane, i-capped primers ukusuka kwi-host cell RNA transcripts, ethi ke isebenzise i-polymerase-catalyzed synthesis ye-viral mRNAs efunekayo.I-polymerase subunit ibophelela kumamkeli pre-mRNAs kwii-5' caps zazo, emva koko umsebenzi we-endonuclease we-polymerase udala ukucandeka kwayo "emva kwe-10-13 nucleotides".Ngaloo ndlela, indlela yayo yahlukile kwii-neuraminidase inhibitors ezifana ne-Oseltamivir kunye ne-Zanamivir.
I-Baloxavir Marboxil yi-inhibitor ekhethiweyo ye-influenza cap-dependent endonuclease ethintela umsebenzi we-polymerase kwaye ngoko ke i-influenza virus mRNA replication 5, 3. Ibonise umsebenzi wonyango ngokuchasene nomkhuhlane A kunye nosulelo lwe-virus ye-B, kubandakanywa neentlobo ezixhathisayo kwii-antiviral agents zangoku 1. Eli chiza inqanda i-enzayimi efunekayo kuphindaphindo lwentsholongwane, ngaloo ndlela iphatha ngokukhawuleza usulelo lwentsholongwane yomkhuhlane 5, Ileyibhile kunye nokunciphisa iimpawu ezinxulumene nosulelo.Idosi enye yale arhente yaboniswa ukuba iphezulu kune-placebo ekudambiseni iimpawu zomkhuhlane kwaye iphezulu kuzo zombini i-oseltamivir kunye neyeza le-placebo kwiziphumo ze-virologic (eziphawulwe ngokuncipha komthamo wentsholongwane egazini).
I-Baroxavir ilungele izigulane ≥ iminyaka eyi-12 ubudala ehlaselwa ngumkhuhlane obukhali ongantsonkothanga kwaye iimpawu zazo zingadluli kwiiyure ezingama-48.Ingqalelo kufuneka ihlawulwe kwimida yeyeza: intsholongwane yomkhuhlane iyatshintsha ngokuhamba kwexesha, kwaye kukho izinto ezifana nohlobo lwentsholongwane kunye ne-subtype.Nje ukuba uxhathiso lwechiza lwentsholongwane kunye ne-pathogenicity yentsholongwane itshintshile, ukusebenza kakuhle kwezonyango kumachiza okuthomalalisa iintsholongwane kunokuba buthathaka.Xa uthatha isigqibo sokuthatha i-basalovir dipivoxil, ulwazi olukhoyo malunga nobuntununtunu bohlobo lwentsholongwane yentsholongwane yengingqi kwichiza kufuneka luthathelwe ingqalelo.
I-Baloxavir Marboxil liyeza lomkhuhlane, i-antiviral, elithathwa njengethamo ledosi enye, ngomlomo, ngabantu abaneminyaka eli-12 ubudala nangaphezulu, ababonise iimpawu zolusulelo isithuba esingadlulanga kwiiyure ezingama-48. I-baloxavir marboxil elawulwa emva kweeyure ezingama-48 ayikavavanywa.
I-Baloxavir Marboxil ayifanele isetyenziswe kunye neemveliso zobisi, iziselo eziqiniswe nge-calcium, okanye i-laxatives, i-antacids, okanye izongezo zomlomo ezine-calcium, isinyithi, i-magnesium, i-selenium, i-aluminium okanye i-zinc.
Iziphumo ebezingalindelekanga eziqhelekileyo ezilandela idosi enye ye-baloxavir marboxil ziquka urhudo, ibronchitis, ukubanda okuqhelekileyo, intloko ebuhlungu, kunye nesicaphucaphu.Izehlo ezingalunganga zixelwe kwi-21% yabantu abafumene i-baloxavir, i-25% yabo bafumana i-placebo, kunye nama-25% e-Oseltamivir.
Patent yaseJapan iJP6212678 ichaze indlela yokudityaniswa kweBaloxavir Marboxil.I-3, i-4-difluorobenzoic acid isetyenziswe njengento eluhlaza ukuze iphendule nge-DMF phantsi kwesenzo se-LDA ukufumana i-2-formyl-3, i-4-difluorobenzoic acid.Emva koko yenza i-thioacetal kunye ne-thiophenol, emva koko iyancitshiswa kwaye ihlukaniswe kunye ne-borane ukuze ifumane i-2-phenylthiomethyl -3, i-4-difluorob, i-8-difluorodibenzo [B, e] i-thiazepine -11 (6H) -enye, kwaye ekugqibeleni iqhekeza eliphambili le-thiazepine I-7, i-8-difluoro-6,11-dihydrodibenzo [B, e] i-thiazepine -11-alcohol ifunyenwe phantsi kokunciphisa i-sodium borohydride.Ukusebenzisa i-3-(benzyloxy) -4-oxo-4H-pyran-2-carboxylic acid ukusabela nge-tert-butyl formate emva kwe-esterification ukufumana i-3-(benzyloxy) -1-((tert-butoxycarbonyl) amino) -4-oxo -1, i-4-dihydropyridine-2-methyl formate hydrate, kwaye emva koko nge-2-(2, 2-dimethoxyethoxy) i-ethylamine idlula ukutshintshiselana kwe-urethane, kwaye emva koko ihamba ngebhayisikili phantsi kwesenzo se-methanesulfonic acid ukufumana i-7-(benzyloxy) -3, 4,12,12a-tetrahydro-1H-[1,4] oxazino [3,4-c] pyridino [2,1-f] [1,2,4] triazine -6, 8-dione hemihydrate, ngoko ke ixutywe kunye (R) -tetrahydrofuran -2-formic acid, emva koko i-crystallized kwaye isonjululwe, kwaye ke iqela elincedisayo le-chiral lisuswa ukufumana i-chiral parent ring molecule (R) -7- (benzyloxy) -3,4,12, 12a-tetrahydro-1H-[1,4] oxazino [3,4-c] pyrido [2,1-f] [1,4] Triazine-6, 8-dione.Emva koko i-molecule yomzali engundoqo isetyenziselwa ukutshintshiselana ne-n-hexanol phantsi kwesenzo se-Grignard reagent, kwaye emva koko kunye neqhekeza eliphambili le-thiazepine 7,8-difluoro-6, 11-dihydrodibenzo [B, e] thiazepine -11-alcohol docking. , kwaye ekugqibeleni i-debutylation kunye ne-condensation nge-methyl chloroformate ukufumana imveliso yokugqibela i-Baloxavir Marboxil.