Enantioselective Synthesis of <i>N</i>-Alkylamines through β-Amino C–H Functionalization Promoted by Cooperative Actions of B(C<sub>6</sub>F<sub>5</sub>)<sub>3</sub> and a Chiral Lewis Acid Co-Catalyst
作者:Yejin Chang、Min Cao、Jessica Z. Chan、Cunyuan Zhao、Yuankai Wang、Rose Yang、Masayuki Wasa
DOI:10.1021/jacs.0c13200
日期:2021.2.10
seemingly competitive Lewisacids, B(C6F5)3, and a chiral Mg- or Sc-based complex, promotes the highly enantioselective union of N-alkylamines and α,β-unsaturated compounds. An array of δ-amino carbonyl compounds was synthesized under redox-neutral conditions by enantioselective reaction of a N-alkylamine-derived enamine and an electrophile activated by the chiral Lewisacid co-catalyst. The utility
[EN] PYRAZOLE DERIVATIVES, COMPOSITIONS AND THERAPEUTIC USE THEREOF<br/>[FR] DÉRIVÉS DE PYRAZOLE, COMPOSITIONS LES COMPRENANT ET LEUR UTILISATION THÉRAPEUTIQUE
申请人:HOFFMANN LA ROCHE
公开号:WO2017191098A1
公开(公告)日:2017-11-09
Compounds of Formula (I): and salts thereof, and methods of use as Janus kinase inhibitors are described herein.
Method for producing allyl compound, and ether or ester compound produced thereby
申请人:MITSUBISHI CHEMICAL CORPORATION
公开号:US20040147757A1
公开(公告)日:2004-07-29
A method for producing an allyl compound having a compositional formula different from that of an allyl starting material compound, which comprises reacting the allyl starting material compound with an oxygen nucleophilic agent in the presence of a catalyst containing at least one transition metal compound containing a transition metal selected from the group consisting of transition metals belonging to Group 8 to Group 10 of the Periodic Table and a multidentate phosphite compound.
Design, Synthesis, and Evaluation of 5′-Diphenyl Nucleoside Analogues as Inhibitors of the Plasmodium falciparum dUTPase
作者:Shahienaz E. Hampton、Beatriz Baragaña、Alessandro Schipani、Cristina Bosch-Navarrete、J. Alexander Musso-Buendía、Eliseo Recio、Marcel Kaiser、Jean L. Whittingham、Shirley M. Roberts、Mikhail Shevtsov、James A. Brannigan、Pia Kahnberg、Reto Brun、Keith S. Wilson、Dolores González-Pacanowska、Nils Gunnar Johansson、Ian H. Gilbert
DOI:10.1002/cmdc.201100255
日期:2011.10.4
Deoxyuridine 5'-triphosphate nucleotidohydrolase (dUTPase) is a potential drug target for malaria. We previously reported some 5'-tritylated deoxyuridine analogues (both cyclic and acyclic) as selective inhibitors of the PlasmodiumfalciparumdUTPase. Modelling studies indicated that it might be possible to replace the trityl group with a diphenyl moiety, as two of the phenyl groups are buried, whereas
[EN] AMINOCYCLOBUTANES AS MONOACYLGLYCEROL LIPASE MODULATORS<br/>[FR] AMINOCYCLOBUTANES SERVANT DE MODULATEURS DE LA MONOACYLGLYCÉROL LIPASE
申请人:JANSSEN PHARMACEUTICA NV
公开号:WO2021191391A1
公开(公告)日:2021-09-30
Aminocyclobutane compounds of Formula (I), and pharmaceutically acceptable salts, isotopes, N-oxides, solvates, and stereoisomers thereof, pharmaceutical compositions containing them, and methods of using them including methods for treating disease states, disorders, and conditions associated with MGL modulation, such as those associated with pain, psychiatric disorders, neurological disorders (including, but not limited to major depressive disorder, treatment resistant depression, anxious depression, autism spectrum disorders, Asperger syndrome, bipolar disorder), cancers and eye conditions: wherein X, R1, R2a, R2b, R3 and R4 are defined herein.