109347-40-2Relevant academic research and scientific papers
Synthesis of Arylacetaldehydes by Iridium-Catalyzed Arylation of Vinylene Carbonate with Arylboronic Acids
Wang, Zhe,Xue, Fei,Hayashi, Tamio
supporting information, p. 11054 - 11057 (2019/07/17)
The one-step synthesis of arylacetaldehydes by carbon–carbon bond formation between formylmethyl and aryl groups has been realized by the reaction of vinylene carbonate with arylboronic acids in the presence of an iridium/bisphosphine catalyst and a catalytic amount of tetrahydroxydiboron.
C8-substituted pyrido[3,4-d]pyrimidin-4(3H)-ones: Studies towards the identification of potent, cell penetrant Jumonji C domain containing histone lysine demethylase 4 subfamily (KDM4)inhibitors, compound profiling in cell-based target engagement assays
Le Bihan, Yann-Va?,Lanigan, Rachel M.,Atrash, Butrus,McLaughlin, Mark G.,Velupillai, Srikannathasan,Malcolm, Andrew G.,England, Katherine S.,Ruda, Gian Filippo,Mok, N. Yi,Tumber, Anthony,Tomlin, Kathy,Saville, Harry,Shehu, Erald,McAndrew, Craig,Carmichael, LeAnne,Bennett, James M.,Jeganathan, Fiona,Eve, Paul,Donovan, Adam,Hayes, Angela,Wood, Francesca,Raynaud, Florence I.,Fedorov, Oleg,Brennan, Paul E.,Burke, Rosemary,van Montfort, Rob L.M.,Rossanese, Olivia W.,Blagg, Julian,Bavetsias, Vassilios
supporting information, p. 316 - 337 (2019/06/05)
Residues in the histone substrate binding sites that differ between the KDM4 and KDM5 subfamilies were identified. Subsequently, a C8-substituted pyrido[3,4-d]pyrimidin-4(3H)-one series was designed to rationally exploit these residue differences between
RETINOID COMPOUND, PREPARATION METHOD THEREFOR, INTERMEDIATES THEREOF AND APPLICATION THEREOF
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Paragraph 0128; 0129, (2019/01/29)
Disclosed are a retinoid compound, a preparation method therefor, intermediates thereof and an application thereof. The retinoid compound I of the present invention has a good tumor growth inhibition rate.
Compound with 2-aminopyrimidine structure as well as preparation method and purpose thereof
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Paragraph 0104-0107, (2019/06/08)
The invention provides a compound of a 2-aminopyrimidine structure shown as a general formula (1), or a stereisomer, enantiomers or medically acceptable salt of the compound, a preparation method of the compound, a medicine composition containing the composition or a purpose of the composition. The compound shown as the general formula (1) can be used for preparing NIK kinase inhibitors, and can be used for preventing and/or treating diseases relevant to NIK kinase, particularly cancer and metabolic diseases, such as B-cell dysfunction related cancer such as multiple myeloma, lymphocyte carcinoma, diffuse large B cell lymphoma of liver cancer, hodgkin lymphoma and chronic lymphocytic leukemia, prostatic cancer, liver cancer, intestinal cancer, medicine induced liver damage, alcohol inducedliver damage, toxic induced acute liver injury, chronic liver inflammation and the like. The general formula (1) is shown in the description.
Peroxygenase-Catalysed Epoxidation of Styrene Derivatives in Neat Reaction Media
Alcalde, Miguel,Arends, Isabel W. C. E.,Hollmann, Frank,Paul, Caroline E.,Rauch, Marine C. R.,Tieves, Florian
, (2019/08/30)
Biocatalytic oxyfunctionalisation reactions are traditionally conducted in aqueous media limiting their production yield. Here we report the application of a peroxygenase in neat reaction conditions reaching product concentrations of up to 360 mM.
Photochemical Homologation for the Preparation of Aliphatic Aldehydes in Flow
Chen, Yiding,Leonardi, Marco,Dingwall, Paul,Labes, Ricardo,Pasau, Patrick,Blakemore, David C.,Ley, Steven V.
, p. 15558 - 15568 (2019/01/04)
Cheap and readily available aqueous formaldehyde was used as a formylating reagent in a homologation reaction with nonstabilized diazo compounds, enabled by UV photolysis of bench-stable oxadiazolines in a flow photoreactor. Various aliphatic aldehydes were synthesized along with the corresponding derivatized alcohols and benzimidazoles. No transition-metal catalyst or additive was required to affect the reaction, which proceeded at room temperature in 80 min.
Biocatalytic Formal Anti-Markovnikov Hydroamination and Hydration of Aryl Alkenes
Wu, Shuke,Liu, Ji,Li, Zhi
, p. 5225 - 5233 (2017/08/17)
Biocatalytic anti-Markovnikov alkene hydroamination and hydration were achieved based on two concepts involving enzyme cascades: epoxidation-isomerization-amination for hydroamination and epoxidation-isomerization-reduction for hydration. An Escherichia coli strain coexpressing styrene monooxygenase (SMO), styrene oxide isomerase (SOI), ω-transaminase (CvTA), and alanine dehydrogenase (AlaDH) catalyzed the hydroamination of 12 aryl alkenes to give the corresponding valuable terminal amines in high conversion (many ≥86%) and exclusive anti-Markovnikov selectivity (>99:1). Another E. coli strain coexpressing SMO, SOI, and phenylacetaldehyde reductase (PAR) catalyzed the hydration of 12 aryl alkenes to the corresponding useful terminal alcohols in high conversion (many ≥80%) and very high anti-Markovnikov selectivity (>99:1). Importantly, SOI was discovered for stereoselective isomerization of a chiral epoxide to a chiral aldehyde, providing some insights on enzymatic epoxide rearrangement. Harnessing this stereoselective rearrangement, highly enantioselective anti-Markovnikov hydroamination and hydration were demonstrated to convert α-methylstyrene to the corresponding (S)-amine and (S)-alcohol in 84-81% conversion with 97-92% ee, respectively. The biocatalytic anti-Markovnikov hydroamination and hydration of alkenes, utilizing cheap and nontoxic chemicals (O2, NH3, and glucose) and cells, provide an environmentally friendly, highly selective, and high-yielding synthesis of terminal amines and alcohols.
Maleimide-assisted anti-Markovnikov Wacker-type oxidation of vinylarenes using molecular oxygen as a terminal oxidant
Nakaoka, Sonoe,Murakami, Yuka,Kataoka, Yasutaka,Ura, Yasuyuki
supporting information, p. 335 - 338 (2016/01/09)
Arylacetaldehydes were successfully synthesized by the anti-Markovnikov Wacker-type oxidation of vinylarenes using 1 atm O2 as a terminal oxidant under mild conditions. Electron-deficient alkenes, such as maleic anhydride and maleimides, were effective additives and would operate as ligands to stabilize the Pd(0) species during the reaction.
Efficient epoxide isomerization within a self-assembled hexameric organic capsule
Caneva, Thomas,Sperni, Laura,Strukul, Giorgio,Scarso, Alessandro
, p. 83505 - 83509 (2016/11/01)
The isomerization of epoxides to the corresponding carbonyl compounds is efficiently catalyzed by the supramolecular organic nano-capsule formed by the self-assembly of six resorcin[4]arene units. The capsule provides a combination of weak Br?nsted acidity and a suitable nano-environment that favors the metal-free isomerization reaction.
Hypoiodite-catalyzed regioselective oxidation of alkenes: An expeditious access to aldehydes in aqueous micellar media
Swamy, Peraka,Reddy, Marri Mahender,Naresh, Mameda,Kumar, Macharla Arun,Srujana, Kodumuri,Durgaiah, Chevella,Narender, Nama
, p. 1125 - 1130 (2015/04/22)
A highly anti-Markovnikov selective oxidation of alkenes based on in situ generated hypoiodite catalysis in aqueous micellar media under mild conditions has been described. This novel catalytic system realizes an efficient synthesis of aldehydes from alkenes in an economically viable and environmentally safe fashion. The preliminary mechanistic studies suggest that the reaction proceeds via tandem iodofunctionalization/1,2-aryl or alkyl migration. The scope and limitations of this tandem process are demonstrated with various mono- and disubstituted (terminal and internal) olefins.
