480449-71-6

Basic information

• Product Name: Edoxaban (TsOH salt)
• Synonyms: Edoxaban (TsOH salt);Edoxaban tosylate;DU-176b;Edoxaban TsOH
• CAS NO: 480449-71-6
• Molecular Formula: C₇H₈O₃S*C₂₄H₃₀ClN₇O₄S
• Molecular Weight: 720.25912
• EINECS: 1592732-453-0
• Mol File: 480449-71-6.mol
• Article Data: 20

Chemical Properties

• Appearance: /
• CAS DataBase Reference: Edoxaban (TsOH salt)(CAS DataBase Reference)
• NIST Chemistry Reference: Edoxaban (TsOH salt)(480449-71-6)
• EPA Substance Registry System: Edoxaban (TsOH salt)(480449-71-6)

Safety Data

• Hazardous Substances Data: 480449-71-6(Hazardous Substances Data)

Usage

Definition

ChEBI: An organosulfonate salt obtained by combining equimolar amounts of edoxaban and 4-toluenesulfonic acid. Used (in the form of its monohydrate) for the treatment of deep vein thrombosis and pulmonary embolism.

Upstream product

• 480449-70-5 edoxaban 
• 104-15-4 toluene-4-sulfonic acid 
• 1445-73-4 1-Methyl-4-piperidone 
• 17899-48-8 2-amino-5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine 
• 480452-36-6 carbamic acid, N-[(1R,2S,5S)-2-[[2-[(5-chloro-2-pyridinyl)amino]-2-oxoacetyl]amino]-5-[(dimethylamino)carbonyl]cyclohexyl]-1,1-dimethylethyl ester 
• 123536-66-3 (1S,4S,5S)-4-iodo-6-oxabicyclo<3.2.1>octan-7-one 
• 720720-96-7 5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxylic acid hydrochloric acid salt 
• 480452-37-7 N¹-[(1S,2R,4S)-2-amino-4-[(dimethylamino)carbonyl]cyclohexyl]-N²-(5-chloro-2-pyridyl)ethanediamide 
• 349125-08-2 ethyl 2-((5-chloropyridin -2-yl)amino)-2-oxoacetate 
• 4771-80-6 1,2,5,6-tetrahydrobenzoic acid 
• 259809-24-0 5-methyl-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine 
• 143150-92-9 2-Bromo-5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]-pyridine 
• 89580-42-7 3-bromo-1-methylpiperidin-4-one hydrobromide 

Relevant articles and documents

Preparation method of edoxaban tosylate and isomers thereof

The invention discloses a preparation method of edoxaban tosylate and isomers thereof. By taking a compound (I) and a compound (II) as starting materials, the method can be used to prepare any one ofhigh-purity edoxaban tosylate (1S, 2R, 4S), edoxaban tosylate enantiomers (1R, 2S, 4R), edoxaban tosylate epimers (1R, 2R, 4S) and edoxaban tosylate epimers (1S, 2S, 4R). Effective guarantee is provided for process research and quality control of the edoxaban tosylate bulk drug and related preparations, the preparation method is suitable for commercialization, the produced edoxaban tosylate bulk drug is high in purity and has great significance and practical value, and the production of the edoxaban tosylate bulk drug and the control of drug quality are facilitated.

Method for the Preparation of Diamine Derivative

The present invention relates to high yield. The present invention relates to a process for preparing high purity ethaboxate p - toluenesulphonate or hydrates thereof. To the present invention, generation of a dielectric toxic substance and a side reaction product can be suppressed, and high yield, high purity of edoxaba p - toluenesulphonate or a hydrate thereof can be advantageously used.

Preparation method of edoxaban

The invention relates to a new preparation route and a new method for a p-toluenesulfonic acid edoxaban hydrate and intermediates thereof. The new method comprises the steps that a high-reactivity compound 109A4x is prepared; a compound 109C6x is prepared by using a new synthesizing method; new compounds 109E8-01, 109E9x and 109T7-01 are prepared; the p-toluenesulfonic acid edoxaban hydrate is prepared by using the intermediates. By using the new method and the new route, the reaction step of copious cooling is omitted, and dangerous elemental sulfur, high-risk n-butyllithium and high-risk azides are prevented from being used. In a word, by means of the method, the p-toluenesulfonic acid edoxaban hydrate and the key intermediates thereof are more easily and safely prepared at a lower coston an industrialization scale.