I-Baloxavir Marboxil CAS 1985606-14-1 API Factory High Quality
I-Shanghai Ruifu Chemical Co., Ltd. ingumkhiqizi ohamba phambili we-Baloxavir Marboxil (CAS: 1985606-14-1) enekhwalithi ephezulu.I-Ruifu Chemical inganikeza ukulethwa komhlaba wonke, intengo encintisanayo, isevisi enhle kakhulu, amanani amancane kanye nenqwaba etholakalayo.Thenga i-Baloxavir Marboxil,Please contact: alvin@ruifuchem.com
Igama Lekhemikhali | I-Baloxavir Marboxil |
Omqondofana | BXM;S-033188 |
Inombolo ye-CAS | 1985606-14-1 |
Isimo Sesitoko | Esitokweni, Isikali Sokukhiqiza Sifika Emakhulwini Amakhilogremu |
I-Molecular Formula | I-C27H23F2N3O7S |
Isisindo samangqamuzana | 571.55 |
Ukuminyana | 1.57±0.10 g/cm3 |
Ukuncibilika | I-Soluble ku-DMSO |
Isitoreji Sesikhathi Eside | Gcina Isikhathi Eside ku -20 ℃ |
I-COA ne-MSDS | Iyatholakala |
Umsuka | Shanghai, China |
Ibhrendi | I-Ruifu Chemical |
Into | Imininingwane |
Ukubukeka | Impushana Emhlophe Kuya Kumhlophe |
Ukuhlonza | I-IR Spectrum ihambisana nezinga lokubhekisela Isikhathi sokugcina sihambisana nezinga lesithenjwa |
Okuqukethwe kwamanzi (nge-KF) | ≤1.0% |
Ukulahlekelwa Ekumisweni | ≤1.0% |
Izinsalela ekushiseni | ≤0.50% |
Izinsimbi Ezisindayo | ≤20ppm |
Izinto Ezihlobene | |
Ukungcola Okukhulu Komuntu Ngamunye | ≤0.50% |
Ukungcola Okuphelele | ≤1.0% |
Usayizi Wezinhlayiyana | I-D90 Dlula i-150um |
I-Chiral Purity | ≥99.0% |
Ubumsulwa | ≥99.0% |
Isivivinyo | 98.0%~102.0% |
Izincibilikisi Ezisele | Ukuthobela Izidingo ze-ICH |
Ukuthumela ngomkhumbi | Ukuthumela Nge-Ice Pack |
Izinga Lokuhlola | I-Enterprise Standard |
Ukusetshenziswa | I-API, ekwelapheni Umkhuhlane A kanye Nezifo Zomkhuhlane B |
Iphakheji:Ibhodlela, isikhwama se-Aluminium foil, 25kg/Cardboard Drum, noma ngokwezidingo zekhasimende.
Isimo Sesitoreji:Gcina isiqukathi sivalwe ngokuqinile futhi usigcine endaweni epholile, eyomile (2~8℃) nengena umoya omuhle kude nezinto ezingahambelani.Vikela ekukhanyeni nakumswakama.
Ukuthumela:Zilethe emhlabeni wonke ngendiza, yi-FedEx/DHL Express.Nikeza ukulethwa okusheshayo nokuthembekile.
I-Baloxavir Marboxil (CAS: 1985606-14-1, BXM, S-033188, Xofluza) iyisidakamizwa esilwa namagciwane esakhiwe yi-Shionogi Co., inkampani yaseJapan eyenza imithi kanye ne-Roche yokwelapha umkhuhlane A kanye nezifo zomkhuhlane B.Umuthi waqale wagunyazwa ukuthi usetshenziswe e-Japan ngo-February 2018 futhi wagunyazwa yi-FDA ngo-Okthoba 24, 2018 ukuze ulaphe umkhuhlane oyingozi kakhulu ezigulini ezineminyaka engu-12 ubudala nangaphezulu ezibe nezimpawu isikhathi esingekho amahora angama-48 Ilebula.I-Baloxavir marboxil, i-cap-endonuclease inhibitor, inendlela ehlukile yokwenza uma iqhathaniswa nesigaba somuthi okhona njengamanje we-neuraminidase inhibitor osetshenziselwa ukwelapha izifo zomkhuhlane.I-Baloxavir Marboxil umuthi omusha wokulwa nomkhuhlane onendlela entsha yokwenza.I-Baloxavir Marboxil iwumkhiqizo we-Baloxavir Acid (S-033447) evimbela ngamandla nangokukhetha i-endonuclease encike ku-cap ngaphakathi kwe-polymerase PA subunit yamagciwane omkhuhlane A no-B, okuholela ekuvinjweni kokulotshwa kwe-RNA nokuphindaphinda.I-Baloxavir nayo isiphenyiwe mayelana namandla ayo okwelapha i-COVID-19 kodwa akukho nzuzo eqinisekisiwe etholakele.
I-Baloxavir Marboxil iyi-ejenti yokwelapha umkhuhlane, ikakhulukazi, inhibitor ye-enzyme eqondise umsebenzi we-endonuclease oncike kugciwane lomkhuhlane, omunye wemisebenzi ye-virus polymerase complex.Ikakhulukazi, ivimbela inqubo eyaziwa ngokuthi i-cap snatching, lapho igciwane lithola ama-primer amafushane, afakwe i-capped kusuka ekubhalweni kweseli ye-RNA ye-host host, elibese liyisebenzisela ukuhlanganiswa kwe-polymerase-catalyzed yama-mRNA adingekayo egciwane.I-polymerase subunit ibophezela kumsingathi wangaphambi kwe-mRNA kumakepisi awo angu-5', bese umsebenzi we-endonuclease we-polymerase uvuselela ukuqhekeka kwawo "ngemuva kwama-nucleotide angu-10–13".Kanjalo, indlela yayo ihlukile kuma-neuraminidase inhibitors njenge-Oseltamivir ne-Zanamivir.
I-Baloxavir Marboxil iyi-inhibitor ekhethiwe ye-influenza cap-dependent endonuclease evimbela ukusebenza kwe-polymerase futhi ngenxa yalokho i-influenza virus mRNA replication 5, 3. Ibonise umsebenzi wokwelapha ngokumelene nezifo ze-influenza A kanye ne-B, kuhlanganise nezinhlobo ezimelana nama-antiviral amanje 1. Lo muthi ivimbela i-enzyme edingekayo ekuphindaphindeni kwegciwane, ngaleyo ndlela yelaphe ngokushesha ukutheleleka ngegciwane lomkhuhlane 5, Ilebula futhi idambise izimpawu ezihambisana nokutheleleka.Umthamo owodwa wale ejenti waboniswa uphakeme kune-placebo ekudambiseni izimpawu zomkhuhlane futhi uphakeme kunawo womabili umuthi we-oseltamivir kanye ne-placebo emiphumeleni ye-virologic (imakwe ngokuncipha kwenani legciwane egazini).
I-Baroxavir ilungele iziguli ezineminyaka engu-≥ engu-12 ubudala ezihlushwa umkhuhlane oyingozi ongaxakile futhi izimpawu zazo zingeqi emahoreni angama-48.Kufanele kuqashelwe ukulinganiselwa kwemithi: igciwane lomkhuhlane liyashintsha ngokuhamba kwesikhathi, futhi kunezici ezifana nohlobo lwegciwane kanye ne-subtype.Uma ukumelana nomuthi kwegciwane kanye ne-pathogenicity yegciwane kushintsha, ukusebenza kahle komtholampilo kwemithi elwa namagciwane kungase kube buthaka.Lapho kunqunywa ukuthi ithathe i-basalovir dipivoxil, ulwazi olutholakalayo mayelana nokuzwela kohlobo lwegciwane lesandulela ngculazi lendawo emuthini kufanele lucatshangelwe.
I-Baloxavir Marboxil umuthi womkhuhlane, i-antiviral, ethathwa njengethebhulethi yomthamo owodwa ngomlomo, ngabantu abaneminyaka engu-12 ubudala noma ngaphezulu, asebeveze izimpawu zalesi sifo isikhathi esingekho amahora angama-48. I-baloxavir marboxil enikezwe ngemuva kwamahora angama-48 ayikahlolwa.
I-Baloxavir Marboxil akufanele inikezwe kanyekanye nemikhiqizo yobisi, iziphuzo eziqiniswe nge-calcium, noma ama-laxative, ama-antacids, noma izithasiselo zomlomo eziqukethe i-calcium, i-iron, i-magnesium, i-selenium, i-aluminium noma i-zinc.
Imiphumela engemihle evamile elandela ukulawulwa komthamo owodwa we-baloxavir marboxil ihlanganisa isifo sohudo, ukucinana kwemigudu yokuphefumula, umkhuhlane ovamile, ikhanda elibuhlungu, nesicanucanu.Izehlakalo ezimbi zibikwe ku-21% wabantu abathole i-baloxavir, u-25% walabo abathola i-placebo, kanye no-25% we-Oseltamivir.
Ilungelo lobunikazi laseJapan i-JP6212678 libike indlela yokuhlanganisa ye-Baloxavir Marboxil.I-3, i-4-difluorobenzoic acid isetshenziswe njengento eluhlaza ukuze kusabelene ne-DMF ngaphansi kwesenzo se-LDA ukuthola i-2-formyl-3, 4-difluorobenzoic acid.Bese yenza i-thioacetal nge-thiophenol, bese iyancishiswa futhi ihlukaniswe ne-borane ukuze ithole i-2-phenylthiomethyl -3, 4-difluorob, 8-difluorodibenzo [B, e] thiazepine -11(6H) -one, futhi ekugcineni isiqephu se-thiazepine esiyinhloko. I-7, 8-difluoro-6,11-dihydrodibenzo [B, e] i-thiazepine -11-alcohol itholakala ngaphansi kokunciphisa i-sodium borohydride.Ukusebenzisa i-3-(benzyloxy)-4-oxo-4H-pyran-2-carboxylic acid ukuze isabele nge-tert-butyl formate ngemva kwe-esterification ukuthola i-3-(benzyloxy) -1-((tert-butoxycarbonyl) amino) -4-oxo -1, 4-dihydropyridine-2-methyl formate hydrate, bese kuthi nge-2-(2, 2-dimethoxyethoxy) i-ethylamine ibhekane ne-urethane exchange reaction, bese ihamba ngebhayisikili ngaphansi kwesenzo se-methanesulfonic acid ukuze ithole 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, ke kuba ihlanganiswe ne-(R) -tetrahydrofuran -2-formic acid, bese i-crystallized futhi ixazululwe, bese iqembu elisizayo le-chiral lisuswa ukuze kutholwe ukhiye we-chiral parent ring molecule (R) -7-(benzyloxy) -3,4,12, I-12a-tetrahydro-1H-[1,4] oxazino [3,4-c] pyrido [2,1-f][1,4] Triazine-6, 8-dione.Khona-ke i-molecule yendandatho engukhiye yomzali isetshenziselwa ukushintshanisa ne-n-hexanol ngaphansi kwesenzo se-Grignard reagent, bese kuba nesiqephu esiyisihluthulelo se-thiazepine 7,8-difluoro-6, 11-dihydrodibenzo [B, e] thiazepine -11-alcohol docking. , futhi ekugcineni ukukhishwa kanye nokujiya nge-methyl chloroformate ukuze kutholwe umkhiqizo wokugcina i-Baloxavir Marboxil.