- Synthetic method of 7-fluoro-5-hydroxy-2,3-dihydro-1hydrogen-indene-1-one
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The invention relates to a synthetic method of 7-fluoro-5-hydroxy-2,3-dihydro-1hydrogen-indene-1-one. The technical problem that there is no synthetic method suitable for industrialization at present is mainly solved. The synthetic method of the invention
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Paragraph 0007
(2019/10/10)
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- Semireduction of alkynoic acids via a transition metal-free α borylation-protodeborylation sequence
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A method for the semi-reduction of alkynoic acids through an α-borylation and subsequent protodeborylation mechanism has been developed. The transition metal-free protocol is achieved through the activation of bis(pinacolato)diboron by an in situ generated carboxylate moiety yielding aryl acrylic acids. Our studies demonstrate an unprecedented dual role for the carboxylate anion that involves the activation of the diboron reagent and a directing effect in the α-borylation.
- Verma, Astha,Grams, R. Justin,Rastatter, Brett P.,Santos, Webster L.
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supporting information
p. 2113 - 2117
(2019/02/25)
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- Synthesis and mesomorphic properties of tolane-based fluorinated liquid crystals with an acrylate linkage
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Six series of tolane-based fluorinated liquid crystals containing an acrylate linker were synthesized and their mesomorphic properties were characterized. The compounds generally exhibit SmA and N phases in wide temperature ranges. The introduction of acrylate linkers increases the clearing points by 20°C-30°C and suppresses the formation of higher ordered monotropic SmB phases. para-Fluorination is favorable for the mesophase stability, whereas meta-fluorination is not. The introduction of a 2,3,5,6-tetrafluorophenylene group decreases the clearing points and also suppresses the formation of the monotropic SmB phase. Copyright Taylor & Francis Group, LLC.
- Chen, Ximin,Shen, Yuehai,Wen, Jianxun
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experimental part
p. 138 - 146
(2011/05/12)
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- Fluorophenyl-substituted alkenylcarboxylic acid guanidides, process for their preparation, their use as a medicament or diagnostic, and medicament containing them
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This invention relates to fluorophenyl-substituted alkenylcarboxylic acid guanidides, process for their preparation, their use as a medicament or diagnostic, and medicament containing them. An embodiment of the invention embraces compounds of the formula I: and the pharmaceutically tolerated salts thereof. The disclosed compounds are valuable inhibitors of the cellular sodium/proton exchanger (Na+/H+ exchanger). They are therefore outstandingly suitable for the treatment of all diseases attributable to increased Na+/H+ exchange.
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- 4-Aralkyl-5-substituted-1,2,4-triazole-5-thiols
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Compounds of formula (I) and pharmaceutically acceptable salts thereof are described in which, n is 0 to 5; X1 to X5 are any accessible combination of hydrogen, halogen, C1 6alkyl, C1 6alkoxy, cyano, nitro, SONH2, SO2NH2, SO2CH3, SO2CH2F, SO2CHF2, SO2CF3, CF3, CHO, OH, CH2OH, CO2H, or CO2CpH2p+1wherein p is 1 to 4; R1 is phenyl substituted by X1 to X5, C1 4alkyl, C3 6cycloalkyl, or an arylC1 4alkyl group substituted by X1 to X5; R2 is hydrogen, C1 4alkyl or (CH2)m-CO2R3; m is 0 to 5; and R3 is H or C1 4alkyl. These compounds are dopamine-β-hydroxylase inhibitors. Pharmaceutical compositions are described as are methods of use. Processes for the preparation of these compounds are described.
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- Dopamine-β-hydroxylase inhibitors and use thereof
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The compounds of this invention are 1-phenylalkyl-2-mercaptotetrazole compounds which are dopamine-β-hydroxylase inhibitors.
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- Cannabis. Part 25. Synthesis of Cannabispirenone-B and its 5,7-Difluoro-analogue
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The naturally occuring cannabispirenone-B (1a) was synthesized by spiroannelation of the piperidine anamine of 5,7-dimethoxyindan-1-carbaldehyde to O-methylcannabispirenone (1b), followed by selective demethylation with lithium iodide in 2,4,6-collidine.I
- Novak, J.,Salemink, C. A.
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p. 2403 - 2406
(2007/10/02)
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