480450-69-9Relevant articles and documents
Preparation method of edoxaban chiral azide intermediate compound
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Paragraph 0009; 0024-0026; 0029-0038, (2021/10/27)
The invention provides a preparation method of an edoxaban chiral azide intermediate compound, which comprises the following steps of: performing substitution reaction on a hydroxyl compound as shown in a formula (II) serving as a substrate and an organic azide compound in an organic solvent in the presence of an amidine structure compound to obtain a chiral azide intermediate compound as shown in a formula (I). A two-step synthesis reaction is directly optimized into one-step reaction synthesis, organic azide compounds such as diphenyl azide phosphate, p-toluenesulfonyl azide and azido trimethylsilane are adopted as sources of azide groups, and a substitution reaction is carried out in a proper solvent under the assistance of amidine structure compounds such as methylimidine, DBN, DBU and trinitrogen amidine to obtain a target compound, namely, a chiral azide intermediate. Not only is the use of highly toxic methylsulfonyl chloride and explosive sodium azide successfully avoided, but also the process difficulty and the production cost are reduced.
Method for preparing eteaban chiral amine intermediate (by machine translation)
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Paragraph 0055-0058, (2020/09/12)
The invention provides a safe and convenient method for preparing N - [(1R, 2S, 5S) -2 - amino -5 - [(dimethylamino) carbonyl] cyclohexyl] carbamic acid tert-butyl formate. The compound N - [(1R, 2R, 5S) -5 - [(dimethylamino) carbonyl] -2 - hydroxycyclohexyl] carbamic acid tert-butyl carbamate and the DBU azidate are then reacted to obtain N - [(1R, 2R, 5S) -5 - [(dimethylamino) carbonyl] cyclohexyl] carbamic acid tert-butyl formate in the presence of DBU to obtain the corresponding amino. N - [(1R, 2S, 5S) -2 - amino -2 -5 - [(dimethylamino) carbonyl] cyclohexyl] carbamic acid tert-butyl formate in the presence of a DBU to obtain the corresponding amino compound. N - 2S [(dimethylamino) carbonyl] cyclohexyl] carbamic acid tert-butyl formate 1R 5S -2 -5 . (by machine translation)
METHOD FOR PRODUCING (1S,4S,5S)-4-BROMO-6-OXABICYCLO[3.2.1]OCTAN-7-ONE
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, (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.