- Preparation of mono-substituted malonic acid half oxyesters (SMAHOs)
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The use of mono-substituted malonic acid half oxyesters (SMAHOs) has been hampered by the sporadic references describing their preparation. An evaluation of different approaches has been achieved, allowing to define the best strategies to introduce diversity on both the malonic position and the ester function. A classical alkylation step of a malonate by an alkyl halide followed by a monosaponification gave access to reagents bearing different substituents at the malonic position, including functionalized derivatives. On the other hand, the development of a monoesterification step of a substituted malonic acid derivative proved to be the best entry for diversity at the ester function, rather than the use of an intermediate Meldrum acid. Both these transformations are characterized by their simplicity and efficiency, allowing a straightforward access to SMAHOs from cheap starting materials.
- Condon, Sylvie,Le Gall, Erwan,Pichon, Christophe,Presset, Marc,Xavier, Tania
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supporting information
p. 2085 - 2094
(2021/09/02)
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- Nano-K2CO3: Preparation, characterization and evaluation of reactive activities
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A novel base, nano-K2CO3, was easily prepared by ultrafine wet milling. The surface properties and the reactive activities of nano-K2CO3 were characterized. It was found that such a base showed higher basicity than normal K2CO3 and could replace sodium (or potassium) alkoxide to carry out monoalkylation and oximation of active methylene compounds. The nano-K2CO3 could be regenarated and reused 10 times without loss of its reactive activity.
- Li, Jun-Zhang,Fan, Shi-Ming,Sun, Xuan-Fei,Liu, Shouxin
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p. 1865 - 1869
(2016/01/20)
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- Intramolecular Schmidt reaction of acyl chlorides with alkyl azides: Preparation of pyrrolizine by intramolecular capture of intermediates with alkenes or alkynes
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The preparation of substituted pyrrolizines through the Schmidt reaction of acyl chlorides with alkyl azides has been realized. Intramolecular capture of the isocyanate ion and N-acyliminium ion intermediates from the Schmidt process with alkene or alkyne
- Wang, Bao-Juan,Xue, Ping,Gu, Peiming
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supporting information
p. 2277 - 2279
(2015/02/05)
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- PEPTIDYLARGININE DEIMINASES (PAD) INHIBITORS
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The present invention relates to compounds of the formula (I): as inhibitors of peptidylarginine deiminases (PADs). It also concerns their use in therapy, particularly in the prophylaxis or treatment of neural injury, and other conditions including cancer, multiple sclerosis, glaucoma, arthritis, rheumatoid arthritis lupus, Alzheimer's disease, and ulcerative colitis.
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Page/Page column 62
(2014/12/12)
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- Creation through immobilization: A new family of high performance heterogeneous bifunctional iminophosphorane (BIMP) superbase organocatalysts
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An immobilized chiral bifunctional iminophosphorane superbase organocatalyst has been developed and applied in a range of challenging enantioselective reactions. A unique feature of this novel catalytic system is that the final step creation of the iminophosphorane occurs at the point of immobilization. The utility of the immobilized catalyst system was demonstrated in the nitro-Mannich reaction of ketimines as well as the conjugate addition of high pKa 1,3-dicarbonyl pro-nucleophiles to nitrostyrene. Catalyst recycling was also demonstrated.
- Goldys, Anna M.,Nez, Marta G.,Dixon, Darren J.
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supporting information
p. 6294 - 6297
(2015/02/05)
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- Copper(II) triflate catalyzed amination and aziridination of 2-Alkyl substituted 1,3-dicarbonyl compounds
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A method to prepare α-acyl-β-amino acid and 2,2-diacyl aziridine derivatives efficiently from Cu(OTf)2 + 1,10-phenanthroline (1,10-phen)-catalyzed amination and aziridination of 2-alkyl substituted 1,3-dicarbonyl compounds with PhI=NTs is described. By taking advantage of the orthogonal modes of reactivity of the substrate through slight modification of the reaction conditions, a divergence in product selectivity was observed. In the presence of 1.2 equiv of the iminoiodane, amination of the allylic C-H bond of the enolic form of the substrate, formed in situ through coordination to the Lewis acidic metal catalyst, was found to selectively occur and give the β-aminated adduct. On the other hand, increasing the amount of the nitrogen source from 1.2 to 2-3 equiv was discovered to result in preferential formal aziridination of the C-C bond of the 2-alkyl substituent of the starting material and formation of the aziridine product.
- Ton, Thi My Uyen,Tejo, Ciputra,Tiong, Diane Ling Ying,Chan, Philip Wai Hong
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experimental part
p. 7344 - 7350
(2012/06/16)
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- Expeditious synthesis of N0-substituted N-mesitylimidazolium salts as NHC precursors
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In contrast to time-consuming, conventional thermal approaches, microwave irradiation provides rapid and convenient access to unsymmetrical N0-substituted N-mesitylimidazolium salts, which are important precursors for NHC ligands used in the construction
- Truscott, Byron J.,Klein, Rosalyn,Kaye, Perry T.
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scheme or table
p. 5041 - 5043
(2011/01/04)
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- LIQUID CRYSTAL COMPOUND COMPRISING TWO CONDENSED AND SUBSTITUTED RINGS
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A new liquid crystal compound comprises two condensed and substituted rings. The ring preferably is a five-membered heterocyclic ring. The heterocyclic ring is preferably condensed with benzene ring or an aromatic six-membered heterocyclic ring. The benzene ring or the aromatic six-membered heterocyclic ring is preferably substituted with a group comprising a cyclic structure and a chain structure. The liquid crystal compound is advantageously used in preparation of a thin phase retarder, such as a wide-ranged l/4 plate, which gives inverse wavelength distribution. The phase retarder can be easily produced according to a simple process by using the new liquid crystal compound.
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Page/Page column 74-76
(2008/06/13)
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- CATHODIC SYNTHESIS OF CYCLOBUTANES
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Cathodic electrolysis of compounds with an activated methylene group in the presence of 1,3-dibromopropane affords 1,1-disubstituted cyclobutanes.
- Vasil'ev, A. A.,Tatarinova, V. I.,Petrosyan, V. A.
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p. 1221 - 1224
(2007/10/02)
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