- PROCESS FOR SYNTHESIZING PHENYLACETIC ACID BY CARBONYLATION OF TOLUENE
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A production process for substituted phenylacetic acids or ester analogues thereof is disclosed. In this process toluene or toluene substituted with various substituents, an alcohol, an oxidant and carbon monoxide are used as raw materials to obtain compounds comprising structure of phenylacetic acid ester or analogues thereof by catalysis of the complex catalyst formed from transition metal and ligand, and such compounds are hydrolyzed to obtain various substituted phenylacetic acid based compounds. This type of compounds and their derivatives serve as important fine chemicals used widely in the industries of pharmaceuticals, pesticides, perfume and the like.
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Paragraph 0050; 0051
(2013/11/19)
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- Palladium-catalyzed oxidative carbonylation of benzylic C-H bonds via nondirected C(sp3)-H activation
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A new strategy for generating benzylpalladium reactive species from toluenes via nondirected C(sp3)-H activation has been developed. This led to construction of an efficient Pd-catalyzed reaction protocol for the oxidative carboxylation of benzylic C-H bonds to form substituted 2-phenylacetic acid esters and derivatives from inexpensive, commercially available starting materials.
- Xie, Pan,Xie, Yinjun,Qian, Bo,Zhou, Han,Xia, Chungu,Huang, Hanmin
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supporting information; experimental part
p. 9902 - 9905
(2012/08/08)
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- Practical synthesis of 2-arylacetic acid esters via palladium-catalyzed dealkoxycarbonylative coupling of malonates with aryl halides
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A new palladium-based system was developed that catalyzes the coupling of aryl halides with diethyl malonates in the presence of mild bases. In the course of the reaction, the intermediately formed diethyl arylmalonate is directly converted into the arylacetic acid ester via liberation of carbon dioxide and an alkanol. This cross-coupling/dealkoxycarbonylation process provides an efficient and high-yielding synthetic entry to diversely functionalized arylacetic acid esters. Two complementary protocols were developed, one of which is optimal for electron-rich, the other for electron-poor aryl halides. Both make use of low loadings of palladium(0) bis(dibenzylideneacetone) (0.5 mol%)/tri-tert-butylphosphonium tetrafluoroborate (1.1 mol%) as the catalyst and diethyl malonate as the reaction solvent. The new procedures are particularly effective for sterically hindered substrates. Copyright
- Song, Bingrui,Rudolphi, Felix,Himmler, Thomas,Goossen, Lukas J.
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supporting information; experimental part
p. 1565 - 1574
(2011/08/03)
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- Design, synthesis and in vivo hypoglycemic activity of tetrazole-bearing N-glycosides as SGLT2 inhibitors
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Novel tetrazole-bearing N-glycosides have been designed and synthesized as SGLT2 inhibitors via a conventional protocol starting from substituted phenylacetic acids and two monosaccharides, D-glucose and D-galactose, and their hypoglycemic activity has been tested in vivo by mice oral glucose tolerance test (OGTT). Two compounds are found to be more potent than the positive control Dapagliflozin. The structure-activity relationship has also been investigated.
- Gao,Zhao,Liu,Shao,Wang,Tang,Wang
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experimental part
p. 1499 - 1508
(2011/02/22)
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- Growth hormone secretagogues
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What is disclosed are growth hormone secretagogues, and their uses, of the formula wherein R1 is C6H5CH2OCH2—, C6H5(CH2)3— or indol-3-ylmethyl; Y is pyrrolidin-1-yl, 4-C1-C6alkylpiperidin-1-yl or NR2R2; R2 are each independently a C1to C6alkyl; R3 is 2-napthyl or phenyl para-substituted by W; W is H, F, CF3, C1-C6alkoxy or phenyl; and R4 is H or CH3, or a pharmaceutically acceptable salt or solvate thereof.
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Page column 70
(2010/02/09)
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- 1,2-disubstituted-6-oxo-3-phenyl-piperidine-3-carboxamides and combinatorial libraries thereof
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The invention relates to combinatorial libraries containing two or more novel piperidine-3-carboxamide derivative compounds, methods of preparing the piperidine-3-carboxamide derivative compounds and piperidine-3-carboxamide derivative compounds bound to a resin
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- LIQUID CRYSTAL MATERIALS WITH SULFUR ATOMS INCORPORATED IN THE PRINCIPAL STRUCTURE: 2. NEW LIQUID CRYSTAL COMPOUNDS; 2-SUBSTITUTED-5-(p-SUBSTITUTED PHENYL)-1,3-DITHIANES.
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2-Substituted-5-(p-substituted phenyl)-1,3-dithianes (8), new liquid crystals, were synthesized. The mesomorphic properties of these compounds were compared with those of the corresponding 2-(p-substituted phenyl)-5-alkyl-1,3-dithianes (9). The main diffe
- Haramoto,Akazawa,Kamogawa
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p. 3173 - 3176
(2007/10/02)
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