52924-55-7Relevant academic research and scientific papers
Imidazo ring PAR4 antagonist and medical applications thereof
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, (2020/01/12)
The invention relates to an imidazo ring compound represented by formula (I) or formula (II), or a pharmaceutically acceptable salt or ester or solvate thereof. The compound disclosed by the inventioncan be used for preparing medicines for preventing or treating thromboembolic diseases.
Substituent Effects and Mechanism in a Mechanochemical Reaction
Barbee, Meredith H.,Kouznetsova, Tatiana,Barrett, Scott L.,Gossweiler, Gregory R.,Lin, Yangju,Rastogi, Shiva K.,Brittain, William J.,Craig, Stephen L.
, p. 12746 - 12750 (2018/10/15)
We report the effect of substituents on the force-induced reactivity of a spiropyran mechanophore. Using single molecule force spectroscopy, force-rate behavior was determined for a series of spiropyran derivatives substituted with H, Br, or NO2/sub
Method for preparing 5-halogen-2,3-dihydroxy benzaldehyde
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Paragraph 0021; 0025; 0026, (2018/11/22)
The invention discloses a method for preparing 5-halogen-2,3-dihydroxy benzaldehyde. The method comprises the following steps: enabling 5-halogen-2-hydroxyl-3-methoxybenzaldehyde to generate ether bond cracking reaction at a temperature from -20 DEG C to
Synthesis of two naturally occurring 3-methyl-2,5-dihydro-1-benzoxepin carboxylic acids
Yamaguchi, Seiji,Tsuchida, Nao,Miyazawa, Masahiro,Hirai, Yoshiro
, p. 7505 - 7511 (2007/10/03)
Two naturally occurring 3-methyl-2,5-dihydro-1-benzoxepin carboxylic acids, 6-hydroxy-3-methyl-8-(phenylethyl)-2,5-dihydro-1-benzoxepin-9-carboxylic acid (radulanin E) (1) and 9-hydroxy-3-methyl-2,5-dihydro-1-benzoxepin-7-carboxylic acid (2), were synthes
Development of a scalable process for CI-1034, an endothelin antagonist
Jacks, Thomas E.,Belmont, Daniel T.,Briggs, Christopher A.,Horne, Nicole M.,Kanter, Gerald D.,Karrick, Greg L.,Krikke, James J.,McCabe, Richard J.,Mustakis, Jason G.,Nanninga, Thomas N.,Risedorph, Guy S.,Seamans, Ronald E.,Skeean, Richard,Winkle, Derick D.,Zennie, Thomas M.
, p. 201 - 212 (2013/09/04)
A concise, convergent multikilogram synthesis of CI-1034 (1), a potent endothelin receptor antagonist, is described. A 15-step preparation from commercially available o-vanillin and benzenesulfonyl chloride employs a remarkably robust Suzuki coupling between a boronic acid and an aromatic sulfonate ester as the key synthetic step. A scalable route capable of producing multikilogram quantities of CI-1034 with no chromatographic steps is described in this contribution. Improvements to the process included using a 4-fluorobenzenesulfonate ester as a suitable substitute for the triflate group in the Suzuki reaction and the use of MgCl2 as a substitute for TiCl4 in a Dieckmann condensation to provide the benzothiazine dioxide core.
Certain benzothiazine dioxide endothelin antagonists and processes for their preparation
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, (2008/06/13)
The instant invention is a series of benzothiazine dioxides, or a pharmaceutically acceptable salt thereof, which are potent endothelin A antagonists with profound in vitro activity, and improved syntheses for the Formula 1 The compounds are useful in treating elevated levels of endothelin, essential renovascular malignant and pulmonary hypertension, cerebral infarction, cerebral ischemia, congestive heart failure, and subarachnoid hemorrhage.
