バロキサビルマルボキシル化学構造式

バロキサビルマルボキシル

化学名:バロキサビルマルボキシル

CAS番号.1985606-14-1

英語名:Baloxavir marboxil

CBNumberCB63361382

MFC27H23F2N3O7S

MW571.55

MOL File1985606-14-1.mol

别名

バロキサビルマルボキシル

バロキサビルマルボキシル (JAN)

バロキサビル　マルボキシル

バロキサビルマルボキシル物理性質

沸点	712.8±70.0 °C(Predicted)
比重(密度)	1.57±0.1 g/cm3(Predicted)
貯蔵温度	Sealed in dry,Store in freezer, under -20°C
溶解性	DMSO:45.0(Max Conc. mg/mL);78.73(Max Conc. mM)
外見	A crystalline solid
酸解離定数(Pka)	-1.46±0.40(Predicted)
色	White to yellow
InChIKey	HKVHAHZGMLTCDW-BWFGELNCSA-N
SMILES	C(O)(=O)OC(OC1=C2N(C=CC1=O)N([C@H]1C3=CC=C(F)C(F)=C3CSC3=CC=CC=C31)[C@]1([H])COCCN1C2=O)C

危険有害性情報のコード(GHS)

バロキサビルマルボキシル化学特性,用途語,生産方法

効能
抗ウイルス薬, キャップ依存性エンドヌクレアーゼ阻害薬
商品名
ゾフルーザ (塩野義製薬)
使用
Baloxavir Marboxil is a prodrug of S-033447, which is an inhibitor of the cap-dependent endonuclease of influenza A and B viruses.
製造方法
The synthesis of baloxavir marboxil involved the following steps: The coupling of the 1-R and 2 fragments was carried out under dehydration conditions of 1-propanephosphonic anhydride (T3P) and methanesulfonic acid at 70 °C to obtain protected baloxavir 19. Compound 19 was then reacted with 0.6 equivalents of PhBr and K2CO3. Debenzylation was then carried out using LiCl in CH3CONMe2 to give baloxavir acid in 94% yield. In the final step for the preparation of the prodrug, baloxavir acid was reacted with chloromethyl methyl carbonate in dimethylacetamide in 93% yield to form baloxavir marboxyl.

The reaction mechanism for the final step for the synthesis of baloxavir marboxil(BXM).
brand name
XOFLUZA? (baloxavir marboxil)
作用機序
Baloxavir marboxil is an influenza therapeutic agent, specifically, an enzyme inhibitor targeting the influenza virus' cap-dependent endonuclease activity, one of the activities of the virus polymerase complex. In particular, it inhibits a process known as cap snatching, by which the virus derives short, capped primers from host cell RNA transcripts, which it then uses for polymerase-catalyzed synthesis of its needed viral mRNAs. A polymerase subunit binds to the host pre-mRNAs at their 5' caps, then the polymerase's endonuclease activity catalyzes its cleavage "after 10–13 nucleotides". As such, its mechanism is distinct from neuraminidase inhibitors such as oseltamivir and zanamivir.
副作用
Common side effects following the single dose administration of baloxavir marboxil include diarrhea, bronchitis, common cold, headache, and nausea. Adverse events were reported in 21% of people who received baloxavir, 25% of those receiving placebo, and 25% of oseltamivir.

バロキサビルマルボキシル上流と下流の製品情報

バロキサビルマルボキシル生産企業

バロキサビルマルボキシルスペクトルデータ(MS)

1985606-14-1, バロキサビルマルボキシルキーワード

Send Inquriy

バロキサビルマルボキシル

危険有害性情報のコード(GHS)

バロキサビルマルボキシル 化学特性,用途語,生産方法

バロキサビルマルボキシル 上流と下流の製品情報

バロキサビルマルボキシル 生産企業

バロキサビルマルボキシル スペクトルデータ(MS)

1985606-14-1, バロキサビルマルボキシル キーワード

バロキサビルマルボキシル化学特性,用途語,生産方法

バロキサビルマルボキシル上流と下流の製品情報

バロキサビルマルボキシル生産企業

バロキサビルマルボキシルスペクトルデータ(MS)

1985606-14-1, バロキサビルマルボキシルキーワード