67976-82-3Relevant articles and documents
Preparation method of edoxaban
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Paragraph 0091-0093, (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.
METHOD FOR PRODUCING (1S,4S,5S)-4-BROMO-6-OXABICYCLO[3.2.1]OCTAN-7-ONE
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Paragraph 0085; 0086, (2015/12/26)
It is an object of the present invention to provide a method for efficiently producing (1S,4S,5S)-4-bromo-6-oxabicyclo[3.2.1]octan-7-one (1), which is important as an intermediate compound for the production of an FXa-inhibiting compound. A method for producing (1S,4S,5S)-4-bromo-6-oxabicyclo[3.2.1]octan-7-one (1), which comprises treating an (R)-α-phenylethylamine salt of (S)-3-cyclohexene-1-carboxylic acid with 1,3-dibromo-5,5-dimethylhydantoin or N-bromosuccinimide in a solvent.
Process for the preparation of pleuromutilins
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Page/Page column 25, (2012/01/11)
A process for the preparation of a compound of formula in the form of a single stereoisomer, comprising deprotecting the amine group in an N-protected amino-hydroxy-cyclohexylsulfanyl-acetyl-mutilin of formula wherein R is an amine protecting group in the form of a single stereoisomer, and isolating a compound of formula I in the form of a single stereoisomer obtained from the reaction mixture; compounds obtainable by such processes, e.g. a compound of formula I in a crystalline form, or salts of a compound of formula I in crystalline form, and processes for the preparation of intermediates for the production of a compound of formula I.