929693-35-6Relevant academic research and scientific papers
Preparation method of Edoxaban tosylate intermediate and intermediate compound
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Paragraph 0021; 0025-0027, (2019/07/04)
The invention provides a preparation method of an Edoxaban tosylate intermediate, the method comprises the following reaction steps: step a, under a certain temperature condition, adding dimethylformamide substituted cyclohexane, triphenylphosphine (PPh3)) and diethyl azodicarboxylate (DEAD) in a solvent, and then adding N-(t-butyloxycarboryl) p-nitrobenzenesulfonamide or N-(t-butyloxycarboryl) p-toluene sulfonamide for reacting to obtain a chirally-turned compound 2; and step b, removing Boc under a strong acid condition so as to obtain a compound 1; the invention further provides intermediate compounds of the compound 1 and the compound 2 in the preparation of the Edoxaban tosylate intermediate; the amino introduction process in the preparation method is simple, the reaction conversion rate is relatively high, and industrialization is easy to realize, so that the use of hazardous chemical sodium azide is avoided, the process safety is improved, and the production yield is improved.
Preparation method of edoxaban
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, (2019/07/08)
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.
Processes for the Preparation of Edoxaban and Intermediates Thereof
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, (2018/07/15)
The present invention provides processes for the preparation of Edoxaban (1) and salts thereof, as well as intermediates thereof. In particular, intermediate compounds and/or salts of the Formulae (3), (4), (6-A), (7-A), (8-A), (9-A) and (10-AS) are provided.
PREPARATION METHOD OF OPTICALLY ACTIVE DIAMINE COMPOUND
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, (2016/02/12)
The problem to be solved is to provide a method for efficiently producing compounds (1) and (1a) that are important intermediate compounds in the production of FXa inhibitors (X) and (X-a). The solutions thereto are a method for producing a compound represented by the formula (8d) using a stereoselective intramolecular cyclization reaction, and a method for producing a compound (1f) or a salt thereof, or a hydrate thereof, which is characterized by desulfonylation of the compound (8d). In each formula, R4a represents a C1-C6 alkyl group, a benzyl group, etc.
A method for producing an optically active Dimamine deriv.
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, (2016/10/09)
The problem to be solved is to provide a method for efficiently producing compounds (1) and (1a) that are important intermediate compounds in the production of FXa inhibitors (X) and (X-a). The solutions thereto are a method for producing a compound represented by the formula (8d) using a stereoselective intramolecular cyclization reaction, and a method for producing a compound (If) or a salt thereof, or a hydrate thereof, which is characterized by desulfonylation of the compound (8d). In each formula, R 4a represents a C1-C6 alkyl group, a benzyl group, etc.
