67976-82-3Relevant academic research and scientific papers
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.
An efficient stereoselective synthesis of six stereoisomers of 3, 4-diaminocyclohexane carboxamide as key intermediates for the synthesis of factor Xa inhibitors
Wang, Xin,Ma, Mingliang,Reddy, Alavala Gopi Krishna,Hu, Wenhao
, p. 1381 - 1388 (2017/02/18)
An efficient stereoselective route for the preparation of six stereoisomers of tert-butyl ((1R, 2S, 5S)-2-amino-5-(dimethylcarbamoyl)cyclohexyl)carbamate 1 starting from simple 3-cyclohexene-1-carboxylic acid has been described. Stereochemistry of the tit
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.
Enantiomerically pure amines
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Page/Page column 15, (2011/12/12)
A compound of formula wherein PROT, PROT' and R have various meanings, processes for its production and production of intermediates in stereoisomerically pure form, and its use for the production of pharmaceutically active compounds.
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.
PROCESS FOR PRODUCING OPTICALLY ACTIVE CARBOXYLIC ACID
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, (2011/10/12)
It has been demanded to provide a process for industrially producing an intermediate for a compound that exhibits an inhibitory effect on activated blood coagulation factor X and is useful as a preventive and/or therapeutic agent for thrombotic diseases. The present invention provides a process for producing the (R-α-phenylethylamine salt of (S)-3-cyclohexene-1-carboxylic acid, comprising reacting 3-cyclohexene-1-carboxylic acid and (R)-α-phenylethylamine using a mixed solvent of water and acetone or a mixed solvent of water and ethyl acetate as a solvent.
