- Chemoselective Synthesis of N -(Aminoalkyl/amidino)phenyl Naphthalene-1-carboxamides and 5,6,7,8-Tetrahydronaphthalene-1-carboxamides and Their Anticoagulant Screening
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N -[(Aminoalkyl)phenyl]-1-naphthamides and N -[(aminoalkyl)phenyl]-5,6,7,8-tetrahydronaphthalene-1-carboxamides were selectively synthesized from the corresponding cyanonaphthamides by catalytic hydrogenation. N -(Amidinophenyl)-1-naphthalenecarboxamides and N -(amidinophenyl)-5,6,7,8-tetrahydronaphthalene-1-carboxamides were chemoselectively obtained from the corresponding O -acetylamidoximes or amidoximes, respectively, by catalytic hydrogenation. The products were screened for their anticoagulant effects in human plasma, as measured by the activated partial thromboplastin time and the prothrombin time in vitro. Amidines and 5,6,7,8-tetrahydronaphthamides were more active than aminoalkyl compounds and naphthamides.
- Nguyen, Thi Ha,Ma, Eunsook
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- ION CHANNEL ANTAGONISTS/BLOCKERS AND USES THEREOF
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Provided are ion channel antagonists/blockers and uses thereof. Specifically, it provides the compounds of formula (I) or pharmaceutically acceptable salts, stereoisomers, solvates or prodrugs, preparation method therefor and application thereof. Definition of each group in the formula can be found in the specification for details. Provided is also pharmaceutical composition useful for treatment of heart disease and other ion channel related diseases.
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Page/Page column 22; 43
(2021/06/22)
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- A preparation method of naphthalene husband xilin acid
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The invention discloses a method for preparing nafcillin acid. The method comprises the following steps: (1) chlorinating 2-ethoxy naphthoic acid and excessive amount of sulfoxide chloride to obtain an acyl chloride solution; carrying out distillation at reduced pressure to remove sulfoxide chloride, dissolving residues with dichloromethane, and thus obtaining a mixed solution A; (2) adding triethylamine and dichloromethane in 6-aminopenicillanic acid, stirring until the solution is clear, and thus obtaining a mixed solution B; (3) dropwise adding the mixed solution A in the mixed solution B for condensation reaction, carrying out thermal reaction for 30-90 min after the mixed solution A completely is dropwise added in the mixed solution B, and thus obtaining a mixed solution C; (4) concentrating the mixed solution C to be dry, and thus obtaining a solid mixture D; (5) stirring and dispersing the solid mixture D with a ketone reagent, acidizing with an acidifier, adding an ether reagent to stir, filtering, adding purified water or saturated salt water in filtrate to crystallize, filtering, washing with water, drying, and thus obtaining nafcillin acid. The method has the advantages of being simple in process, easy to operate, simple in postprocessing and high in yield.
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Paragraph 0025; 0026; 0044; 0050
(2017/10/05)
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- Diastereoselective photocycloaddition using memory effect of molecular chirality controlled by crystallization
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Naphthamides derived from L-proline, which exist as a mixture of several diastereomers in solution, converged to single diastereomer by crystallization, and the conformational transformation was controlled after the crystals were dissolved in the solvent at low temperature, where the frozen conformation was retained long enough for subsequent asymmetric reaction. The Royal Society of Chemistry.
- Sakamoto, Masami,Unosawa, Atsushi,Kobaru, Shuichiro,Hasegawa, Yasuhiro,Mino, Takashi,Kasashima, Yoshio,Fujita, Tsutomu
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p. 1632 - 1634
(2008/02/10)
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