5445-22-7Relevant academic research and scientific papers
KINASE INHIBITOR
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Paragraph 0185; 0186, (2021/04/16)
The present invention aims to provide a novel kinase inhibitor and the like, and a therapeutic agent for a disease, a drug discovery screening method and the like utilizing such inhibitor and the like. The compound represented by the following formula (I) and a salt thereof can inhibit plural kinases including LATS (particularly LATS2) which is the major kinase in the Hippo signal transduction pathway. In addition, diseases or tissue damage associated with failure of cellular proliferation can be treated. Therefore, the present invention is beneficial, for example, in the research field of cell functions and diseases, in which the Hippo signal transduction pathway is involved, and the like. Furthermore, it is beneficial in the medical field for the treatment of such diseases and the like. wherein each symbol is as defined in the DESCRIPTION.
ADDITIVE COMPOSITION FOR CULTURE MEDIUM, ADDITIVE COMPOUND FOR CULTURE MEDIUM, AND METHOD FOR CULTURE OF CELLS OR TISSUE USING SAME
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Paragraph 0168-0169, (2020/06/15)
The present invention provides a medium additive composition containing a compound represented by the following formula (I), or a salt thereof: {wherein each symbol is as defined in the DESCRIPTION.}
One-pot oxidative bromination – Esterification of aldehydes to 2-bromoesters using cerium (IV) ammonium nitrate and lithium bromide
Nikishin, Gennady I.,Kapustina, Nadezhda I.,Sokova, Lyubov L.,Bityukov, Oleg V.,Terent'ev, Alexander O.
supporting information, p. 352 - 354 (2017/01/03)
A two-step, one-pot reaction of aldehydes with the CAN/LiBr oxidation system under solvent-free conditions followed by the addition of methanol affords methyl α-bromocarboxylates. The oxidation of aldehydes with methanol using this system gives only methyl esters. A facile method, which does not require special equipment, was developed for the synthesis of 2-bromoesters from aliphatic aldehydes with carbon chain lengths of 5–10 atoms.
Enantioselective construction of tetrasubstituted stereogenic carbons through bronsted base catalyzed michael reactions: α′-hydroxy enones as key enoate equivalent
Badiola, Eider,Fiser, Bla,Gmez-Bengoa, Enrique,Mielgo, Antonia,Olaizola, Iurre,Urruzuno, Iaki,Garca, Jess M.,Odriozola, Jos M.,Razkin, Jess,Oiarbide, Mikel,Palomo, Claudio
supporting information, p. 17869 - 17881 (2015/02/19)
Catalytic and asymmetric Michael reactions constitute very powerful tools for the construction of new C-C bonds in synthesis, but most of the reports claiming high selectivity are limited to some specific combinations of nucleophile/electrophile compound types, and only few successful methods deal with the generation of all-carbon quaternary stereocenters. A contribution to solve this gap is presented here based on chiral bifunctional Bronsted base (BB) catalysis and the use of α′-oxy enones as enabling Michael acceptors with ambivalent H-bond acceptor/donor character, a yet unreported design element for bidentate enoate equivalents. It is found that the Michael addition of a range of enolizable carbonyl compounds that have previously demonstrated challenging (i.e., α-substituted 2-oxindoles, cyanoesters, oxazolones, thiazolones, and azlactones) to α′-oxy enones can afford the corresponding tetrasubstituted carbon stereocenters in high diastereo- and enantioselectivity in the presence of standard BB catalysts. Experiments show that the α′-oxy ketone moiety plays a key role in the above realizations, as parallel reactions under identical conditions but using the parent α,β-unsaturated ketones or esters instead proceed sluggish and/or with poor stereoselectivity. A series of trivial chemical manipulations of the ketol moiety in adducts can produce the corresponding carboxy, aldehyde, and ketone compounds under very mild conditions, giving access to a variety of enantioenriched densely functionalized building blocks containing a fully substituted carbon stereocenter. A computational investigation to rationalize the mode of substrate activation and the reaction stereochemistry is also provided, and the proposed models are compared with related systems in the literature.
Enzymatic lactonization stategy for enantioselective synthesis of a tetrahydrolipstatin synthon
Sharma,Chattopadhyay
, p. 8059 - 8062 (2007/10/03)
A novel lipase-catalyzed protocol has been formulated for the simultaneous enantiocontrol of three stereogenic centers in a flexible acyclic system. This involved a porcine pancreatic lipase (PPL)-catalyzed δ- lactonization of a racemic 3,5-dihydroxy-2-alkyl ester to produce the lactone with high enantioselectivity (92.8%). The product lactone and its analogues are useful synthons for the asymmetric synthesis of various bioactive compounds, which include the potential anti-obesity compound, tetrahydrolipstatin.
A convenient route for the homologation of saturated esters to α,β-unsaturated esters
Mohan, H Rama,Rao, A S
, p. 698 - 700 (2007/10/02)
Methyl hexanoate (1a) is transformed to methyl 2-hydroxyheptanoate (5a) employing the following sequence of reactions (Scheme 1); (i) reaction with sodium hydride-dimethyl sulfoxide, (ii) Pummerer rearrangement with acetic anhydride-sodium acetate, (iii) alkaline hydrolysis and (iv) esterification with diazomethane.The α-hydroxy ester (5a) is converted into methyl 2E-heptenoate (7a) employing the following reactions (Scheme 2); (i) reaction with phosphorous tribromide and (ii) elimination using DBU.Thus, the sequence of reactions given in Schemes 1 and 2 provide aconvenient route for the one carbon homologation of saturated esters to α,β-unsaturated esters.
Synthesis and Structure Elucidation of γ-Aminobutyric Acid Conjugates with Lipidic Acids, Lipidic Amino Acids and Lipidic Peptides
Hussain, Rohanah,Toth, Istvan,Gibbons, William A.
, p. 963 - 966 (2007/10/02)
A series of γ-aminobutyric acid esters of lipidic acids, lipidic peptides and γ-aminobutyric acid amides of lipidic α-amino acids and oligomers were synthesised.The GABA conjugates with ester linkages (6j-r) were prepared by coupling the lipidic acids and peptide conjugates to the carboxyl terminus of GABA.Two types of GABA conjugates linked by amide bonds were synthesised.This class included compounds 5d-f in which the amino group of the lipidic amino acid is condensed with the carboxyl function of GABA and compounds 7a-b with the carboxyl terminus of the α-amino acid coupled to the amino group of GABA.The lipidic amino acid peptide oligomers were varied from 1-3 units, and the alkyl side chains ranged from 5-17 carbon atoms in length in order to impart different lipophilicities to the GABA molecule conjugates. Key Words: Amino acids, fatty / Peptides, lipidic / Lipophilic GABA conjugates / Drug delivery
SOLVOLYSIS OF 1-CHLORO-1-ALKENYL PHENYL SULFIDES. SYNTHESIS OF α-BROMO PHENYL THIOCARBOXYLIC ESTERS, α-BROMO ALKYL CARBOXYLIC ESTERS AND α-PHENYLTHIO METHYL CARBOXYLIC ESTERS
Fortes, C. C.,Chaves, M. H.
, p. 751 - 762 (2007/10/02)
1-Chloro-1-alkenyl phenyl sulfides treated with bromine followed by hydrolysis or methanolysis give α-bromo phenyl thiocarboxylic esters and α-phenylthio methyl carboxylic esters.Direct oxidative solvolysis with bromine and alcohol give α-bromo alkyl carboxylic esters.
ONE POT SYNTHESIS OF α-BROMO AND α-IODO KETONES FROM EPOXIDES
Denis, J. N.,Krief, A.
, p. 1429 - 1430 (2007/10/02)
α-bromo and α-iodo ketones are obtained in good yield and in one pot by reaction of terminal and disubstituted epoxides with trimthylsilyl halides and further oxidation (CrO3/H2SO4).
