Baloxavir Marboxil CAS 1985606-14-1 API Ụlọ ọrụ dị elu
Shanghai Ruifu Chemical Co., Ltd. bụ onye na-emepụta Baloxavir Marboxil (CAS: 1985606-14-1) nwere àgwà dị elu.Ruifu Chemical nwere ike ịnye nnyefe zuru ụwa ọnụ, ọnụahịa asọmpi, ọrụ magburu onwe ya, obere na nnukwu ọnụọgụ dị.Ịzụta Baloxavir Marboxil,Please contact: alvin@ruifuchem.com
Aha Chemical | Baloxavir Marboxil |
Ụdị okwu | BXM;S-033188 |
Nọmba CAS | 1985606-14-1 |
Ọnọdụ Ahịa | Na Akụrụngwa, Mpụta Ihe ruru narị narị kilograms |
Usoro ihe omimi | C27H23F2N3O7S |
Ibu molekụla | 571.55 |
Njupụta | 1.57±0.10 g/cm3 |
Solubility | Soluble na DMSO |
Nchekwa ogologo oge | Na-echekwa ogologo oge na -20 ℃ |
COA & MSDS | Dị |
Mmalite | Shanghai, China |
Ụdị | Ruifu Chemical |
Ihe | Nkọwapụta |
Ọdịdị | Ọcha ka Gbanyụọ-Ọcha ntụ ntụ |
njirimara | Spectrum IR dabara na ọkọlọtọ ntụaka Oge njide dabara na ọkọlọtọ ntụaka |
Ọdịnaya mmiri (nke KF) | ≤1.0% |
Ọnwụ na ihicha | ≤1.0% |
Ihe fọdụrụ na mgbanye | ≤0.50% |
Ọla dị arọ | ≤20ppm |
Ihe ndị emetụtara | |
Kachasị adịghị ọcha nke onye | ≤0.50% |
Mgbakọta adịghị ọcha | ≤1.0% |
Nha urughuru | D90 gafere 150um |
Chiral ịdị ọcha | ≥99.0% |
Ịdị ọcha | ≥99.0% |
Nyocha | 98.0% ~ 102.0% |
Ihe mgbaze fọdụrụnụ | Soro ICH chọrọ |
Mbupu | Mbupu na ngwugwu ice |
Nlele ọkọlọtọ | Standardkpụrụ ụlọ ọrụ |
Ojiji | API, na ọgwụgwọ nke Influenza A na Influenza B |
ngwugwu:Kalama, Aluminom foil bag, 25kg / Cardboard Drum, ma ọ bụ dị ka ndị ahịa chọrọ.
Ọnọdụ Nchekwa:Debe akpa ahụ nke ọma ma chekwaa n'ebe dị jụụ, kpọrọ nkụ (2 ~ 8 ℃) yana ụlọ nkwakọba ihe nke ọma na-esi na ihe ndị na-adabaghị adaba.Chebe site na ìhè na mmiri mmiri.
Mbupu:Jiri ikuku na-ebuga ụwa niile site na FedEx / DHL Express.Nye nnyefe ngwa ngwa na ntụkwasị obi.
Baloxavir Marboxil (CAS: 1985606-14-1, BXM, S-033188, Xofluza) bụ ọgwụ mgbochi nje nke Shionogi Co., ụlọ ọrụ ọgwụ Japan na Roche mepụtara maka ọgwụgwọ nke influenza A na influenza B.A kwadoro ọgwụ ahụ na mbụ maka ojiji na Japan na February 2018 ma kwadoro FDA na October 24, 2018 maka ọgwụgwọ nke nnukwu ọrịa influenza na-enweghị mgbagwoju anya na ndị ọrịa 12 afọ na ndị okenye bụ ndị nwere akara ngosi maka ihe karịrị awa 48 Label.Baloxavir marboxil, onye na-egbochi okpu-endonuclease, nwere usoro pụrụ iche nke ime ihe ma e jiri ya tụnyere klas ọgwụ neuraminidase inhibitor dị ugbu a nke a na-eji agwọ ọrịa influenza.Baloxavir Marboxil bụ ọgwụ mgbochi influenza ọhụrụ nwere usoro ihe ọhụrụ.Baloxavir Marboxil bụ prodrug nke Baloxavir Acid (S-033447) na ike na nhọrọ na-egbochi endonuclease na-adabere okpu n'ime polymerase PA subunit nke influenza A na B nje, na-eduga na mgbochi nke RNA transcription na mmegharị.A nyochakwara Baloxavir maka ike ọ nwere ịgwọ COVID-19 mana ọ nweghị uru egosipụtara achọpụtara.
Baloxavir Marboxil bụ onye na-ahụ maka ọgwụgwọ influenza, kpọmkwem, onye na-egbochi enzyme na-elekwasị anya na ọrụ endonuclease na-adabere na influenza nje, otu n'ime ọrụ nke nje polymerase complex.Karịsịa, ọ na-egbochi usoro a maara dị ka ịpụnara okpu, nke nje ahụ na-enweta mkpụmkpụ, mkpuchi mkpuchi site na transcript cell cell RNA, nke ọ na-eji eme ihe maka njikọ polymerase-catalyzed nke mRNA viral ọ chọrọ.Otu subunit polymerase na-ejikọta na pre-mRNA ndị ọbịa na okpu 5' ha, mgbe ahụ, ọrụ endonuclease nke polymerase na-eme ka nkwụsị ya "mgbe 10-13 nucleotides gasịrị".N'ihi ya, usoro ya dị iche na neuraminidase inhibitors dị ka Oseltamivir na Zanamivir.
Baloxavir Marboxil bụ onye na-ahọrọ inhibitor nke influenza okpu na-adabere endonuclease nke na-egbochi ọrụ polymerase na ya mere influenza virus mRNA replication 5, 3. O gosila ọgwụgwọ ọgwụgwọ megide influenza A na B nje nje, gụnyere nsogbu na-eguzogide ọgwụ mgbochi ugbu a 1. Ọgwụ a. na-egbochi enzyme achọrọ maka mmeghari nje, si otú a na-agwọ ọrịa nje flu ngwa ngwa 5, Label na ibelata mgbaàmà ndị metụtara ọrịa.E gosiputara otu dose nke onye ọrụ a ka ọ dị elu karịa placebo n'ịkwụsị mgbaàmà influenza ma dị elu karịa ma oseltamivir na placebo ọgwụ na nsonaazụ virologic (nke a na-ebelata ibu viral).
Baroxavir dị mma maka ndị ọrịa ≥ 12 afọ ndị nwere nnukwu influenza na-enweghị mgbagwoju anya na mgbaàmà ya anaghị agafe awa 48.Ekwesịrị ịṅa ntị na njedebe nke ọgwụ: nje influenza na-agbanwe ka oge na-aga, na e nwere ihe ndị dị ka ụdị nje na subtype.Ozugbo mgbochi ọgwụ nje na nje nje na-agbanwe agbanwe, nrụpụta ụlọ ọgwụ nke ọgwụ nje nwere ike ịdalata.Mgbe ị na-ekpebi ma ị ga-ewere basalovir dipivoxil, a ga-atụle ozi dị na uche nke nje nje na-efe efe mpaghara na ọgwụ ahụ.
Baloxavir Marboxil bụ ọgwụ influenza, ọgwụ nje, nke a na-ewere dị ka otu mbadamba mbadamba, site n'ọnụ, site n'aka ndị mmadụ dị afọ 12 ma ọ bụ karịa, nke gosipụtara mgbaàmà nke ọrịa a karịa awa 48. baloxavir marboxil a na-enye mgbe awa iri anọ na asatọ anwalebeghị.
E kwesịghị ijikọ Baloxavir Marboxil na ngwaahịa mmiri ara ehi, ihe ọṅụṅụ na-edozi calcium, ma ọ bụ laxatives, antacids, ma ọ bụ ihe mgbakwunye ọnụ nwere calcium, iron, magnesium, selenium, aluminum ma ọ bụ zinc.
Mmetụta ndị a na-ahụkarị na-esochi otu dose nke baloxavir marboxil gụnyere afọ ọsịsa, bronchitis, oyi nkịtị, isi ọwụwa, na ọgbụgbọ.A kọrọ ihe ọjọọ na 21% nke ndị natara baloxavir, 25% nke ndị na-anata placebo, na 25% nke Oseltamivir.
Patent Japanese JP6212678 kọrọ usoro njikọ nke Baloxavir Marboxil.3, 4-difluorobenzoic acid ejiri mee ihe dị ka akụrụngwa iji meghachi omume na DMF n'okpuru ọrụ LDA iji nweta 2-formyl-3, 4-difluorobenzoic acid.Mgbe ahụ, ọ na-etolite thioacetal na thiophenol, mgbe ahụ, a na-ebelata ma kewaa ya na borane iji nweta 2-phenylthiomethyl -3, 4-difluorob, 8-difluorodibenzo [B, e] thiazepine -11 (6H) - otu, na n'ikpeazụ isi thiazepine iberibe. 7, 8-difluoro-6,11-dihydrodibenzo [B, e] thiazepine -11 mmanya na-enweta n'okpuru mbelata nke sodium borohydride.Iji 3- (benzyloxy) -4-oxo-4H-pyran-2-carboxylic acid meghachi omume na tert-butyl formate mgbe esterification nweta 3- (benzyloxy) -1- ((tert-butoxycarbonyl) amino) -4-oxo -1, 4-dihydropyridine-2-methyl formate hydrate, na mgbe ahụ na 2- (2, 2-dimethoxyethoxy) ethylamine na-enweta mmeghachi omume mgbanwe urethane, wee cyclizes n'okpuru ọrụ nke methanesulfonic acid iji nweta 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, mgbe ahụ ọ bụ. condensed na (R) -tetrahydrofuran -2-formic acid, mgbe ahụ crystallized na kpebie, na mgbe ahụ, chiral auxiliary otu wepụrụ iji nweta isi chiral nne na nna mgbanaka 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.Mgbe ahụ, a na-eji molekul nne na nna mgbanaka isi mee mgbanwe na n-hexanol n'okpuru ọrụ Grignard reagent, wee jiri mkpịsị ugodi thiazepine 7,8-difluoro-6, 11-dihydrodibenzo [B, e] thiazepine -11-docking mmanya. , na n'ikpeazụ debutylation na condensation na methyl chloroformate iji nweta ikpeazụ ngwaahịa Baloxavir Marboxil.