- Preparation method 3 -aldehyde -5 -methylbenzoic acid
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The invention belongs to the technical field of organic synthesis, and particularly relates to a preparing method of 3-formyl group-5-methylbenzoid acid. According to the preparing method, 3-bromine-5-methylbenzaldehyde serves as a raw material, 3-bromine-5-methylbenzaldehyde reacts with alcohol to prepare acetal, acetal is subjected to a lithium-halogen exchanging reaction with a lithiation reagent to prepare a phenyl lithium compound, the phenyl lithium compound is reacted with carbon dioxide, then 3-formyl group-5-methylbenzoid acid is obtained through decomposition of diluted hydrochloricacid, finally through purification, 3-formyl group-5-methyl benzoic acid is obtained, and the reacted solvent is tetrahydrofuran. The preparing method of 3-formmyl group-5-methylbenzoid acid has the advantages that raw materials are cheap and easy to obtain, the reaction condition is mild, the aftertreatment operation is simple, the production cost is low, the reaction cost is lowered, and the preparing method is suitable for industrialized production.
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Paragraph 0018; 0020; 0023; 0025; 0028; 0030
(2020/08/14)
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- Novel S1P1 receptor agonists - Part 4: Alkylaminomethyl substituted aryl head groups
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In a previous communication we reported on the discovery of alkylamino pyridine derivatives (e.g. 1) as a new class of potent, selective and efficacious S1P1 receptor (S1PR1) agonists. However, more detailed profiling revealed that this compound class is phototoxic in vitro. Here we describe a new class of potent S1PR1 agonists wherein the exocyclic nitrogen was moved away from the pyridine ring (e.g. 11c). Further structural modifications led to the identification of novel alkylaminomethyl substituted phenyl and thienyl derivatives as potent S1PR1 agonists. These new alkylaminomethyl aryl compounds showed no phototoxic potential. Based on their in vivo efficacy and ability to penetrate the brain, the 5-alkyl-aminomethyl thiophenes appeared to be the most interesting class. Potent and selective S1PR1 agonist 20e, for instance, maximally reduced the blood lymphocyte count (LC) for 24 h after oral administration of 10 mg/kg to rat and its brain concentrations reached >500 ng/g over 24 h.
- Lescop, Cyrille,Müller, Claus,Mathys, Boris,Birker, Magdalena,De Kanter, Ruben,Kohl, Christopher,Hess, Patrick,Nayler, Oliver,Rey, Markus,Sieber, Patrick,Steiner, Beat,Weller, Thomas,Bolli, Martin H.
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supporting information
p. 222 - 238
(2016/04/20)
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- Imidazopyridine-based fatty acid synthase inhibitors that show anti-HCV activity and in vivo target modulation
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Potent imidazopyridine-based inhibitors of fatty acid synthase (FASN) are described. The compounds are shown to have antiviral (HCV replicon) activities that track with their biochemical activities. The most potent analogue (compound 19) also inhibits rat FASN and inhibits de novo palmitate synthesis in vitro (cell-based) as well as in vivo.
- Oslob, Johan D.,Johnson, Russell J.,Cai, Haiying,Feng, Shirley Q.,Hu, Lily,Kosaka, Yuko,Lai, Julie,Sivaraja, Mohanram,Tep, Samnang,Yang, Hanbiao,Zaharia, Cristiana A.,Evanchik, Marc J.,McDowell, Robert S.
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supporting information
p. 113 - 117
(2013/02/26)
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- NOVEL AMINOMETHYL BENZENE DERIVATIVES
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The invention relates to novel aminomethyl benzene derivatives, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunomodulating agents. (I) wherein A represents one of the groups (I), (I), (I) and
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Page/Page column 42; 43
(2009/10/22)
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- N-acetonylbenzamides and their use as fungicides
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Certain N-acetonylbenzamides exhibit low phytotoxicity and are useful for control of a wide range of fungi, including phytopathogenic fungi of the classes Oomycetes, Ascomycetes, Deuteromycetes and Basidiomycetes.
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