929693-35-6Relevant articles and documents
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.
Processes for the Preparation of Edoxaban and Intermediates Thereof
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Paragraph 0251; 0252, (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.
A method for producing an optically active Dimamine deriv.
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Paragraph 0189-0191, (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.