- Imidazo ring PAR4 antagonist and medical applications thereof
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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.
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- Substituent Effects and Mechanism in a Mechanochemical Reaction
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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
- Barbee, Meredith H.,Kouznetsova, Tatiana,Barrett, Scott L.,Gossweiler, Gregory R.,Lin, Yangju,Rastogi, Shiva K.,Brittain, William J.,Craig, Stephen L.
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p. 12746 - 12750
(2018/10/15)
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- Method for preparing 5-halogen-2,3-dihydroxy benzaldehyde
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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
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Paragraph 0021; 0025; 0026
(2018/11/22)
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- Synthesis of two naturally occurring 3-methyl-2,5-dihydro-1-benzoxepin carboxylic acids
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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
- Yamaguchi, Seiji,Tsuchida, Nao,Miyazawa, Masahiro,Hirai, Yoshiro
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p. 7505 - 7511
(2007/10/03)
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- Development of a scalable process for CI-1034, an endothelin antagonist
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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.
- 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.
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p. 201 - 212
(2013/09/04)
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- Certain benzothiazine dioxide endothelin antagonists and processes for their preparation
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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.
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