75590-19-1Relevant articles and documents
Radical-mediated aerobic oxidation of substituted styrenes and stilbenes
Aman, Hasil,Chiu, Wei-Hua,Chuang, Gary Jing,Liu, Pin-Heng
supporting information, p. 20103 - 20106 (2021/12/02)
A 2,2-azobis(isobutyronitrile)-catalyzed oxidative cleavage of alkenes with molecular oxygen as the oxidant was described. Carbonyl compounds and oxiranes were obtained in moderate yield under mild conditions. This study provided useful insights into the mechanism of aerobic oxidative cleavage of alkenes.
METHODS OF PROMOTING BETA CELL PROLIFERATION
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Paragraph 00203, (2018/06/30)
The present disclosure provides methods of promoting proliferation of a pancreatic cell. The methods are useful for the treatment of diabetes and other diseases characterized by impaired glucose tolerance.
THIENOPYRIMIDINE AND THIENOPYRIDINE COMPOUNDS AND METHODS OF USE THEREOF
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Paragraph 00475, (2016/04/20)
The present disclosure provides compounds and methods for inhibiting the interaction of menin with its upstream or downstream signaling molecules including but not limited to MLL1, MLL2 and MLL-fusion oncoproteins. Compounds of the disclosure may be used
β-tert-Butyl aspartate as an organocatalyst for the asymmetric α-amination of α,α-disubstituted aldehydes
Theodorou, Alexis,Papadopoulos, Giorgos N.,Kokotos, Christoforos G.
supporting information, p. 5438 - 5443 (2013/07/05)
The enantioselective α-amination reaction of α,α- disubstituted aldehydes can lead to a variety of enantioenriched amino aldehydes, amino alcohols, and amino acids. After screening a variety of amino acids and their derivatives, we identified a cheap, simple, commercially available aspartic acid derivative that can catalyze efficiently the reaction between α,α-disubstituted aldehydes and dialkyl azodicarboxylates. The reaction proceeds smoothly leading to the corresponding α-aminated adducts in moderate to quantitative yields and moderate to high enantioselectivities (up to 96% ee). Finally, the conversion of these adducts to α,α-disubstituted quaternary amino acids is also described.
Efficient catalytic Corey-Chaykovsky reactions involving ketone substrates
Kavanagh, Sarah A.,Piccinini, Alessandro,Connon, Stephen J.
supporting information; experimental part, p. 2089 - 2093 (2010/11/04)
It has been demonstrated for the first time that a sulfide catalyst, utilised at 20 mol% loading, can promote methylene transfer to ketones in the presence of methyl triflate and an organic base. This metal-free methodology is of broad scope-both aliphatic and aromatic ketones (including trifluoromethyl ketones) can be converted to synthetically useful terminal epoxides in excellent yields at room temperature.
Microbiological transformations 43. Epoxide hydrolases as tools for the synthesis of enantiopure α-methylstyrene oxides: A new and efficient synthesis of (S)-ibuprofen
Cleij,Archelas,Furstoss
, p. 5029 - 5035 (2007/10/03)
Biohydrolysis of various α-methylstyrene oxide derivatives, differently substituted at the aromatic ring, was investigated using 10 epoxide hydrolases from different origins. Our results indicate that the enantioselectivity of these biohydrolyses strongly depends on the nature of the enzyme and of the substituent. Using some of these enzymes, this approach allows to prepare these epoxides in high optical purity. The potentiality to perform efficient preparative-scale resolution using such a biocatalyst was illustrated by the four-step synthesis of (S)-ibuprofen, a nonsteroidal antiinflammatory drug and household pain killer, one of the top-ten drugs sold worldwide. Using a combined chemoenzymatic strategy, we were thus able to set up a four-step enantioconvergent procedure allowing for the synthesis of this compound in optically pure form and with a 47% overall yield, including the resolution process, due to a possible recycling of the formed diol via chemical racemisation.
