365997-31-5Relevant articles and documents
Preparation method of edoxaban tosylate and isomers thereof
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Paragraph 0071; 0079-0080, (2021/02/06)
The invention discloses a preparation method of edoxaban tosylate and isomers thereof. By taking a compound (I) and a compound (II) as starting materials, the method can be used to prepare any one ofhigh-purity edoxaban tosylate (1S, 2R, 4S), edoxaban tosylate enantiomers (1R, 2S, 4R), edoxaban tosylate epimers (1R, 2R, 4S) and edoxaban tosylate epimers (1S, 2S, 4R). Effective guarantee is provided for process research and quality control of the edoxaban tosylate bulk drug and related preparations, the preparation method is suitable for commercialization, the produced edoxaban tosylate bulk drug is high in purity and has great significance and practical value, and the production of the edoxaban tosylate bulk drug and the control of drug quality are facilitated.
SALT OF AMINE-PROTECTED (1S,2R,4S)-1,2-AMINO-N,N-DIMETHYLCYCLOHEXANE-4-CARBOXAMIDE
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Page/Page column 21, (2018/02/20)
Disclosed are compounds and methods for the preparation of Edoxaban. In particular, a camphor sulfonate salt of an amine-protected [(1R,2S,5S)-1,2-amino-5-[(dimethylamino)carbonyl] cyclohexane, an intermediate that may be formed in the synthesis of Edoxaban, is disclosed as well as methods of its preparation.
Discovery of N-[(1R,2S,5S)-2-{[(5-chloroindol-2-yl)carbonyl]amino}-5-(dimethylcarbamoyl)cyclohexyl]-5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxamide hydrochloride: A novel, potent and orally active direct inhibitor of factor Xa
Nagata, Tsutomu,Yoshino, Toshiharu,Haginoya, Noriyasu,Yoshikawa, Kenji,Nagamochi, Masatoshi,Kobayashi, Syozo,Komoriya, Satoshi,Yokomizo, Aki,Muto, Ryo,Yamaguchi, Mitsuhiro,Osanai, Ken,Suzuki, Makoto,Kanno, Hideyuki
experimental part, p. 1193 - 1206 (2009/08/08)
In the early 1990's, we reported on the low-molecular selective fXa inhibitor DX-9065a having two amidino groups. However, it had poor oral bioavailability due to its strong basic amidino groups. To obtain fXa inhibitors with improved oral bioavailability