- Preparation method of 5, 7-dichloro-1, 2, 3, 4-tetrahydroisoquinoline
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The invention provides a preparation method of 5, 7-dichloro-1, 2, 3, 4-tetrahydroisoquinoline. The preparation method comprises the following steps: preparing a compound A by taking 3, 5-dichlorobenzoic acid as a raw material; preparing a compound B from the compound A; preparing a compound C from the compound B; preparing a compound D from the compound C; and obtaining a white solid 5, 7-dichloro-1, 2, 3, 4-tetrahydroisoquinoline from the compound D. The preparation method of 5, 7-dichloro-1, 2, 3, 4-tetrahydroisoquinoline provided by the invention has the advantages of high product purity and high product yield.
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Paragraph 0019; 0023; 0026; 0034-0035; 0039; 0046-0047
(2021/02/06)
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- Synthesis method of lifitegrast intermediate 5,7-dichloro-1,2,3,4-tetrahydroisoquinoline
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The invention discloses a synthesis method of a lifitegrast intermediate 5,7-dichloro-1,2,3,4-tetrahydroisoquinoline, wherein the synthesis method comprises the steps: by using 2,4-dichlorobenzaldehyde as a starting material, carrying out nitro-alcohol co
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Paragraph 0086-0087; 0089
(2020/05/05)
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- ROCK KINASE INHIBITORS
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The present invention relates to compounds that inhibit ROCK activity. In particular, the present invention relates to compounds, pharmaceutical compositions and methods of use, such as methods of inhibiting ROCK activity and methods for treating, for example cerebral cavernous malformation syndrome (CCM) and cardiovascular diseases using the compounds and pharmaceutical compositions of the present invention.
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Paragraph 0172-0173; 0175
(2020/05/29)
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- Molecularly engineered Ru(II) sensitizers compatible with cobalt(II/III) redox mediators for dye-sensitized solar cells
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Thiocyanate-free isoquinazolylpyrazolate Ru(II) complexes were synthesized and applied as sensitizers in dye-sensitized solar cells (DSCs). Unlike most other successful Ru sensitizers, Co-based electrolytes were used, and resulting record efficiency of 9.53% was obtained under simulated sunlight with an intensity of 100 mW cm-2. Specifically, dye 51-57dht.1 and an electrolyte based on Co(phen)3 led to measurement of a JSC of 13.89 mA cm-2, VOC of 900 mV, and FF of 0.762 to yield 9.53% efficiency. The improved device performances were achieved by the inclusion of 2-hexylthiophene units onto the isoquinoline subunits, in addition to lengthening the perfluoroalkyl chain on the pyrazolate chelating group, which worked to increase light absorption and decrease recombination effects when using the Co-based electrolyte. As this study shows, Ru(II) sensitizers bearing sterically demanding ligands can allow successful utilization of important Co electrolytes and high performance.
- Wu, Kuan-Lin,Huckaba, Aron J.,Clifford, John N.,Yang, Ya-Wen,Yella, Aswani,Palomares, Emilio,Gr?tzel, Michael,Chi, Yun,Nazeeruddin, Mohammad Khaja
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supporting information
p. 7388 - 7395
(2016/08/06)
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- LFA-1 INHIBITOR AND POLYMORPH THEREOF
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Methods of preparation and purification of a compound, intermediates thereof, a polymorph thereof, and related compounds are disclosed. Formulations and uses thereof in the treatment of LFA -1 mediated diseases are also disclosed.
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Paragraph 00113; 00115
(2014/02/16)
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- Novel Organic Light Emitting Materials
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Novel phosphorescent metal complexes containing 2-phenylisoquinoline ligands with at least two substituents on the isoquinoline ring are provided. The disclosed compounds have low sublimation temperatures that allow for ease of purification and fabrication into a variety of OLED devices.
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Page/Page column
(2013/06/27)
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- A Pd(II)-catalyzed ring-expansion reaction of cyclic 2-azidoalcohol derivatives: Synthesis of azaheterocycles
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(Chemical Equation Presented) A Pd(II)-catalyzed ring expansion-reaction of cyclic 2-azidoalcohol derivatives was found to proceed via an unprecedented C-C bond cleavage-C-N bond formation sequence, providing substituted azaheterocycles.
- Chiba, Shunsuke,Xu, Yan-Jun,Wang, Yi-Feng
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supporting information; experimental part
p. 12886 - 12887
(2009/12/06)
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- Inhibitors of phenylethanolamine N-methyltransferase and epinephrine biosynthesis: I. Chloro-substituted 1,2,3,4-tetrahydroisoquinolines
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In a search for inhibitors of epinephrine biosynthesis as potential therapeutic agents, a series of 13 ring-chlorinated 1,2,3,4-tetrahydroisoquinolines was prepared. These compounds were tested initially for their ability to inhibit rabbit adrenal phenylethanolamine N-methyltransferase (PNMT) in vitro. Enzyme-inhibitor dissociation constants, determined for the six most potent members of the series, indicated the following order of decreasing potency: 7,8-Cl2>6,7,8-Cl3>7-Cl~8-Cl>5,6,7,8-Cl4>5,7,8-Cl3. These compounds were subsequently examined for PNMT-inhibiting activity in intact rats and mice. 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline (SK&F 64139) was the most potent member of the series both in vitro and in vivo and is currently undergoing clinical investigation.
- Bondinell,Chapin,Girard,Kaiser,Krog,Pavloff,Schwartz,Silvestri,Vaidya,Lam,Wellman,Pendleton
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p. 506 - 511
(2007/10/02)
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