- A simple synthetic route to methyl 3-fluoropyridine-4-carboxylate by nucleophilic aromatic substitution
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The nitro group of methyl 3-nitropyridine-4-carboxylate (1) has successfully been replaced by fluoride anion via nucleophilic aromatic substitution to give the 3-fluoropyridine-4-carboxylate 2.
- Tjosaas, Freddy,Fiksdahl, Anne
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- HETEROCYCLIC COMPOUNDS AS MODULATORS OF STIMULATOR OF INTERFERON GENES (STING)
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The present invention relates to compounds of formula (I) and salts, stereoisomers, tautomers or N-oxides thereof that are useful as modulators of STING (Stimulator of Interferon Genes). The present invention further relates to the compounds of formula (I) for use as a medicament and to a pharmaceutical composition comprising said compounds.
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Page/Page column 163-164
(2021/06/22)
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- FUNCTIONALIZED HETEROCYCLIC COMPOUNDS AS MODULATORS OF STIMULATOR OF INTERFERON GENES (STING)
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The present invention relates to compound-linker constructs and antibody-drug-conjugates of compounds of formula (I) that are useful as modulators of STING (Stimulator of Interferon Genes).
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Page/Page column 200
(2021/06/22)
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- Preparation method of 2-trifluoromethyl-3-fluoro-4-picolinic acid and derivatives thereof
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The invention discloses a preparation method of 2-trifluoromethyl-3-fluoro-4-picolinic acid and derivatives thereof, and is characterized in that provided is the preparation method of 2-trifluoromethyl-3-fluoro-4-picolinic acid and the derivatives thereof by a method of introducing trifluoromethyl into 2-site of a polysubstituted pyridine ring through a free radical mechanism, wherein the preparation method is suitable for large-scale application. The method for directly carrying out trifluoromethylation reaction on the 2-site of 3-fluoro-4-pyridine carboxylic acid alkyl ester is reported forthe first time, and is simple and convenient in process, easily available in raw materials, high in conversion rate and simple in reaction post-treatment operation. Meanwhile, the selectivity of the method in introducing trifluoromethyl into the 2-site of pyridine is quite high, and a single product with trifluoromethyl substituted at the 2-site can be obtained only through simple recrystallization.
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Paragraph 0043-0047
(2020/04/17)
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- Spin-Center Shift-Enabled Direct Enantioselective α-Benzylation of Aldehydes with Alcohols
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Nature routinely engages alcohols as leaving groups, as DNA biosynthesis relies on the removal of water from ribonucleoside diphosphates by a radical-mediated "spin-center shift" (SCS) mechanism. Alcohols, however, remain underused as alkylating agents in synthetic chemistry due to their low reactivity in two-electron pathways. We report herein an enantioselective α-benzylation of aldehydes using alcohols as alkylating agents based on the mechanistic principle of spin-center shift. This strategy harnesses the dual activation modes of photoredox and organocatalysis, engaging the alcohol by SCS and capturing the resulting benzylic radical with a catalytically generated enamine. Mechanistic studies provide evidence for SCS as a key elementary step, identify the origins of competing reactions, and enable improvements in chemoselectivity by rational photocatalyst design.
- Nacsa, Eric D.,MacMillan, David W. C.
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supporting information
p. 3322 - 3330
(2018/03/13)
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- TREATMENT OF DISEASES BY EPIGENETIC REGULATION
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The present disclosure provides non-naturally occurring polyphenol compounds that inhibit the bromodomain and extra terminal domain (BET) proteins. The disclosed compositions and methods can be used for treatment and prevention of cancer as well as sepsis
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Paragraph 0313-0314
(2013/11/05)
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- PIPERAZINES AND PIPERIDINES AS mGluR5 POTENTIATORS
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The invention relates to compounds of Formula (I) or pharmaceutically acceptable salts or solvates thereof: wherein Ar1, Ar2, A, X, Y, m, n and R1 to R5 are described in the specification.
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Page/Page column 67
(2008/06/13)
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- PHARMACEUTICAL COMPOSITIONS FOR THE PREVENTION AND TREATMENT OF COMPLEX DISEASES AND THEIR DELIVERY BY INSERTABLE MEDICAL DEVICES
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The present invention relates to polyphenol-like compounds that are useful for inhibiting VCAM-1 expression, MCP-1 expression and/or SMC proliferation in a mammal. The disclosed compounds are useful for regulating markers of inflammatory conditions, including vascular inflammation, and for treatment and prevention of inflammatory and cardiovascular diseases and related disease states.
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Page/Page column 51-52
(2008/06/13)
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