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Rivaroxaban

Rivaroxaban 구조식 이미지
카스 번호:
366789-02-8
상품명:
Rivaroxaban
동의어(영문):
CS-273;Xarelto;Rivaroxaba;Rivaroxban;Rivaroxaban;Rivanoxaban;Rivarobaxan;BAY 59-7939;Rivaroxaban API;(S)-Rivaroxaban
CBNumber:
CB91176772
분자식:
C19H18ClN3O5S
포뮬러 무게:
435.88
MOL 파일:
366789-02-8.mol

Rivaroxaban 속성

녹는점
228-229°C
끓는 점
732.6±60.0 °C(Predicted)
밀도
1.460±0.06 g/cm3(Predicted)
저장 조건
Refrigerator
산도 계수 (pKa)
13.36±0.46(Predicted)

안전

Rivaroxaban C화학적 특성, 용도, 생산

개요

Venous thromboembolism continues to be a major health concern despite conventional anticoagulation therapies. Rivaroxaban is a recent market introduction that directly inhibits FXa with high potency (Ki=0.4 nM; IC50=0.7 nM) and selectivity>10,000-fold over other related serine proteases (thrombin, trypsin, plasmin, FVIIa, FIXa, FXIa, urokinase, and activated protein C). From the X-ray crystal structure, the central oxazolidinone moiety anchors the drug through two hydrogen bonds to Gly219 and directs the morpholinone group into the S4 pocket and the chlorothiophene portion into the S1 pocket. These key components may be coupled together synthetically by a couple of routes. Condensation of 3-morpholinone with 4-fluoronitrobenzene followed by catalytic hydrogenation provides N-(p-aminophenyl)morpholinone for subsequent reaction with (S)-2-(phthalimidomethyl)oxirane. With establishment of the aminoalcohol adduct, cyclization with 1,1′-carbonyldiimidazole generates the central oxazolidinone. Deprotection and acylation with 5-chlorothiophene-2-carbonyl chloride affords rivaroxaban.

화학적 성질

White Solid

Originator

Bayer (Germany)

용도

A novel antithrombotic agent. A highly potent and selective, direct FXa inhibitor

용도

anti-coagulant; Factor X inhibitor,Rivaroxaban is an orally active, direct inhibitor of Factor Xa (Ki = 0.4 nM), which is a crucial component of the intrinsic and extrinsic pathways of the blood coagulation cascade.It demonstrates >10,000-fold greater selectivity for Factor Xa compared to other related serine proteases.In various animal arterial and venous thrombosis models, rivaroxaban is reported to inhibit thrombin formation without prolonging bleeding time and has been approved for clinical use as an anticoagulant in the prevention of stroke and the treatment of venous thromboembolisms.

정의

ChEBI: A monocarboxylic acid amide obtained by formal condensation of the carboxy group of 5-chlorothiophene-2-carboxylic acid with the amino group of 4-{4-[(5S)-5-(aminomethyl)-2-oxo-1,3-oxazolidin-3-yl]phenyl}morpholin-3-one. An anticoagulant u ed for prophylaxis of venous thromboembolism in patients with knee or hip replacement surgery.

상표명

Xarelto

부작용

Regarding safety, there was no statistical difference in the incidence of major postoperative bleeding between any of the rivaroxaban dose groups and enoxaparin although there did appear to be a dose dependency in the rivaroxaban set. In addition to bleeding and subsequent posthemorrhagic anemia, presenting as weakness, paleness, asthenia, dizziness, headache, or unexplained swelling, other common adverse events included nausea, increased GGT, and an increase in transglutaminase. Owing to its mechanism of action, there is a bleeding risk, so the drug is contraindicated in patients with clinically active bleeding. Rivaroxaban is also contraindicated in pregnant and breast-feeding women and in patients with hepatic disease associated with coagulopathy and clinically relevant bleeding risk.

Chemical Synthesis

Rivaroxaban is a recent market introduction that directly inhibits FXa with high potency (Ki 0.4 nM; IC50 0.7 nM) and selectivity, W10,000-fold over other related serine proteases (thrombin, trypsin, plasmin, FVIIa, FIXa, FXIa, urokinase, and activated protein C). From the X-ray crystal structure, the central oxazolidinone moiety anchors the drug through two hydrogen bonds to Gly219 and directs the morpholinone group into the S4 pocket and the chlorothiophene portion into the S1 pocket. These key components may be coupled together synthetically by a couple of routes. Condensation of 3-morpholinone with 4-fluoronitrobenzene followed by catalytic hydrogenation provides N-(p-aminophenyl)morpholinone for subsequent reaction with (S)-2-(phthalimidomethyl)oxirane. With establishment of the aminoalcohol adduct, cyclization with 1,1 -carbonyldiimidazole generates the central oxazolidinone. Deprotection and acylation with 5-chlorothiophene-2-carbonyl chloride affords rivaroxaban. The drug is formulated in 10-mg tablets for once-daily oral administration to patients undergoing elective hip or knee replacement surgery to prevent VTE.

Rivaroxaban 준비 용품 및 원자재

원자재

준비 용품


Rivaroxaban 공급 업체

글로벌( 437)공급 업체
공급자 전화 팩스 이메일 국가 제품 수 이점
Nanjing Gold Pharmaceutical Technology Co. Ltd.
025-84209270 15906146951
025-84209270 wgp@nanjing-pharmaceutical.com CHINA 115 55
Jiangsu Zhongbang Pharmaceutical Co., Ltd.
025-87151996
025-87151996 zbsales@chinaredsun.com CHINA 32 55
Beijing Cooperate Pharmaceutical Co.,Ltd.
+86-10-60279497 +86(0)15646567669
+86-10-60279497 sales01@cooperate-pharm.com CHINA 1817 55
Casorganics US Corp
+17326109938
sales@casorganics.com CHINA 175 58
Nanjing Shizhou Biotechnology Co., Ltd
(+86)18013869214
(+86)25-85563444 rose.shi@synzest.com CHINA 3497 58
Nanjing Shizhou Biotechnology Co., Ltd
(+86)18013869214
(+86)25-85563444 rose.shi@synzest.com CHINA 3497 58
Shanghai Bojing Chemical Co.,Ltd.
+86-21-37122233
+86-21-37127788 Candy@bj-chem.com CHINA 497 55
Henan Tianfu Chemical Co.,Ltd.
0371-55170693
0371-55170693 info@tianfuchem.com CHINA 22625 55
Hangzhou FandaChem Co.,Ltd.
0086 158 5814 5714 (Mobile
+86-571-56059825 fandachem@gmail.com CHINA 3268 55
Nanjing ChemLin Chemical Industry Co., Ltd.
025-83697070
product@chemlin.com.cn CHINA 3014 60

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