- Tetrasubstituted 1,3-Enynes by Gold-Catalyzed Direct C(sp2)-H Alkynylation of Acceptor-Substituted Enamines
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A gold-catalyzed synthesis of tetrasubstituted 1,3-enynes from hypervalent iodine(III) reagents and activated alkenes is reported. This reaction involves an in situ formed alkynyl Au(III) species and a subsequent direct C(sp2)-H functionalization of alkenes, offering 26 enynes in 62-92% yield with excellent functional group tolerance.
- Han, Chunyu,Tian, Xianhai,Zhang, Huili,Rominger, Frank,Hashmi, A. Stephen K.
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supporting information
p. 4764 - 4768
(2021/06/30)
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- Synthesis of Thiazoles and Isothiazoles via Three-Component Reaction of Enaminoesters, Sulfur, and Bromodifluoroacetamides/Esters
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A three-component strategy for the synthesis of thiazoles and isothiazoles has been developed by employing enaminoesters, fluorodibromoiamides/ester, and sulfur. The thiazoles and isothiazoles were formed via two C-F bond cleavages along with the formation of new C-S, C-N, and N-S bonds. The strategy provides high selectivity for the synthesis of thiazoles/isothiazoles, which have vital applications in drug discovery and development.
- Ma, Xingxing,Yu, Xiaoxia,Huang, Hua,Zhou, Yao,Song, Qiuling
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supporting information
p. 5284 - 5288
(2020/07/14)
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- Phenyl substituted dihydropyridine compound and uses thereof
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The present invention relates to a phenyl substituted dihydropyridine compound and uses thereof, further to a pharmaceutical composition containing the compound. According to the present invention, the compound or the pharmaceutical composition can be used as mineralocorticoid receptor antagonists.
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Paragraph 0177; 0185-0187
(2019/05/16)
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- Copper-Catalyzed Tandem Reaction of Enamino Esters with ortho-Halogenated Aromatic Carbonyls: One-Pot Approach to Functionalized Quinolines
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An efficient and practical approach for the synthesis of functionalized quinolines has been developed by using the copper-catalyzed tandem C–C bond formation and C–N coupling reaction of enamino esters and ortho-halogenated aromatic carbonyl compounds. Various functional groups were tolerated under the reaction conditions, and a series of quinolines were easily obtained in moderate to good yields. A gram-scale reaction was also performed to demonstrate a further application of this synthetic method.
- Peng, Fei,Liu, Jin,Li, Lili,Chen, Zhiwei
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supporting information
p. 666 - 672
(2018/02/14)
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- Facile synthesis of pyrido[2,3-d]pyrimidines via cyclocondensation of 4,6-dichloro-2-methylsulfanylpyrimidine-5-carbaldehyde with β-substituted β-aminoacrylic esters
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Abstract A new facile synthesis of pyrido[2,3-d]pyrimidin-4-ones via cyclocondensation of 4,6-dichloro-2-methylsulfanylpyrimidine-5-carbaldehyde with β-alkyl and β-aryl-β-aminoacrylic esters followed by hydrolysis of chlorine atom at position 4 of pyridopyrimidine ring has been developed. The cyclocondensation was found to be accelerated by acid.
- Chizhova, Maria E.,Bakulina, Olga Yu.,Ivanov, Alexander Yu.,Lobanov, Pavel S.,Dar'in, Dmitrii V.
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supporting information
p. 6196 - 6203
(2015/08/03)
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- C1-symmetric bisphosphine ligands and their use in the asymmetric synthesis of pregabalin
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Materials and methods for preparing (S)-(+)-3-(aminomethyl)-5-methyl-hexanoic acid and structurally related compounds via enantioselective hydrogenation of prochiral olefins are disclosed. The methods employ novel chiral catalysts, which include C1-symmetric bisphosphine ligands bound to transition metals.
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Page/Page column 22
(2008/06/13)
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- COMBINATION OF CB2 MODULATORS AND PDE4 INHIBITORS FOR USE IN MEDICINE
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Combination of one or more CB2 modulators such as a compound of formula (I), (II) and (III); and one more PDE4 inhibitors are useful of treating conditions which are mediated by the activity of CB2 receptors or conditions which are mediated by PDE4, such
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Page/Page column 44
(2010/02/13)
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- Highly enantioselective rhodium-catalyzed hydrogenation of β-dehydroamino acid derivatives using monodentate phosphoramidites
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New and very easily accessible monodentate phosphoramidite ligands have been developed that lead to excellent ee's and full conversions in the hydrogenation of (E)- and (Z)-β-dehydroamino acid derivatives with both aliphatic and aromatic side chains. Particularly, two different catalytic systems were established for (E)-β-(acylamino)acrylates (98-99% ee) and (Z)-β-(acylamino)acrylates (92-95% ee) based on phosphoramidites 2 and 3, respectively. Copyright
- Pena, Diego,Minnaard, Adriaan J.,De Vries, Johannes G.,Feringa, Ben L.
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p. 14552 - 14553
(2007/10/03)
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- Rh(I)-catalyzed enantioselective hydrogenation of (E)- and (Z)-beta-(acylamino)acrylates using 1,4-bisphosphine ligands under mild conditions.
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[reaction: see text] Rh-Me-BDPMI (1a) complex can be an effective catalyst for the hydrogenations of (E)- and (Z)-beta-(acylamino)acrylates, in which the Z-isomers hydrogenated with the same or even higher ee values than the corresponding E-isomers. The conversion yield and enantioselectivity of E- and Z-isomers were largely dependent on the solvent, and thus, the E-isomers were hydrogenated more effectively in CH(2)Cl(2), whereas the Z-isomers were hydrogenated more effectively in polar MeOH solvent.
- Lee, Sang-gi,Zhang, Yong Jian
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p. 2429 - 2431
(2007/10/03)
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- Syntheses and Reactions of 2-Halo-5-thiazolecarboxylates
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A variety of 2-halo-5-thiazolecarboxylates was prepared from substituted-3-aminoacrylates and 3-ketoesters.Selective reduction of 2-chloro-5-thiazolecarboxylates 4a, 4i and 4j with sodium borohydride in ethanol provided the corresponding 2-halo-5-thiazolemethanols 27 - 29.Nucleophilic displacement on methyl methanesulfonate (32c) occured selectivity at the 5-substituent to provide 2-chloro-4-(trifluoromethyl)-5-(heteroatom-substituted methyl)thiazoles 32d-f.
- Lee, Len F.,Schleppnik, Francis M.,Howe, Robert K.
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p. 1621 - 1630
(2007/10/02)
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