50347-17-6Relevant articles and documents
HETEROBIFUNCTIONAL MOLECULES AS TEAD INHIBITORS
-
Paragraph 0261-0262; 0277-0278, (2021/09/11)
The invention relates to compounds and methods of using said compounds, as well as pharmaceutical compositions containing such compounds, for treating diseases and conditions mediated by TEAD, such as cancer.
N-Alkylation of Alkylolamines with Alcohols Over Mesoporous Solid Acid–Base Cs–B–Zr Catalyst
Chen, Aimin,Wang, Houyong,Liu, Rui,Bo, Yingying,Hu, Jun
, p. 1182 - 1193 (2016/07/06)
Abstract: The mesoporous solid acid–base Cs–B–Zr mixed oxides were synthesized using the co-precipitation method followed by a subsequent thermal treatment. The catalytic activity of solid Cs–B–Zr mixed oxide was tested for solvent free acid–base catalysed direct alkylolamines with alcohols as green alkylating agent. The effects of Cs/B/Zr ratio, calcination temperature, reaction conditions, and reaction substrate on the catalytic performance of the catalysts were investigated. The XRD, N2 adsorption–desorption, ICP-OES, FT-IR and NH3/CO2-TPD results showed that the mesoporous structure and acid–base properties of the catalysts play important roles in the reaction. A suitable number of acid and basic sites on the catalyst lead to a high activity for the N-alkylation reaction. Graphical Abstract: A direct N-alkylation of amino alcohol with alcohols has been developed using mixed oxide Cs–B–Zr as an acid–base bifunctionalized catalyst.[Figure not available: see fulltext.]
Ligand, metal complex containing ligand, and reaction using metal complex containing ligand
-
Page/Page column 46-50, (2016/10/31)
A hydrogen transfer reaction may be more efficiently promoted by using a metal complex represented by Formula (2): (wherein, R1 to R8 are the same or different, and each represents a hydrogen atom, a substituted or unsubstituted alkyl group or the like; or wherein; R1 and R2, R2 and R3, R3 and R4, R4 and R5, and R5 and R6 are respectively bonded to each other to form a bivalent hydrocarbon group; R9 are the same or different, and each represents an alkyl group or cycloalkyl group; M is ruthenium (Ru) or the like; X is a ligand; and n is 0, 1 or 2). More specifically, the metal complex enables a hydrogenation reaction of various substrates having a stable carbonyl group or the like to be advanced with a high yield under mild conditions.
Catalytic hydrogenation of unactivated amides enabled by hydrogenation of catalyst precursor
Miura, Takashi,Held, Ingmar E.,Oishi, Shunsuke,Naruto, Masayuki,Saito, Susumu
supporting information, p. 2674 - 2678 (2013/06/26)
A general method for catalytic hydrogenation of unactivated amides was achieved. During the catalyst induction period, a novel structural change was observed involving full hydrogenation of the interior unsaturated bonds of the pyridines of the Ru-containing catalyst precursor. Based on this observation, the mechanism of amide hydrogenation may involve a two-step pathway, wherein the Ru catalyst having an H-Ru-N-H functionality is generated in the first step, followed by the amide carbonyl group interacting with the outer, rather than the inner, sphere of the Ru catalyst.
BI-FUNCTIONAL QUINOLINE ANALOGS
-
, (2013/03/26)
Provided are compounds of Formula I: wherein X is: R1 and R2 together with the phenyl to which they are bound may form a bicyclic, fused heterocyclic ring, and all other variables are as defined herein, as well as their use in treating pulmonary inflammation or bronchoconstriction and compositions comprising and processes for preparing the same.
INDANOL DERIVATIVE
-
Page/Page column 84, (2010/11/25)
The present invention provides a compound having the following general formula (I) which is useful as a neurokinin receptor antagonist: (wherein, R1, R2: optionally substituted (hetero)aryl, R3: -CO-R4, -CO-O-R4, etc., R4: alkyl, cycloalkyl, etc., A: CH2, CO, SO2, B: a single bond, etc., D: oxygen, CH2, E: alkylene, alkenylene, n: 1 to 3).
Desilylation procedure via a naphthalene-catalysed lithiation reaction
Behloul, Cherif,Guijarro, David,Yus, Miguel
, p. 6908 - 6915 (2007/10/03)
The reaction of silyl protected alcohols, amines and thiols with lithium powder and a catalytic amount of naphthalene, in THF, at 0°C led, after hydrolysis, to the recovery of the free alcohols, amines and thiols in very good yields. At least a phenyl group was required in the silyl protecting group for the success of the reaction. Some polyfunctionalised starting materials have successfully been deprotected. The stereochemical outcome of the deprotection of a silylated chiral secondary alcohol has also been studied and no racemization was observed. The process has shown to be a good alternative to the acid-catalysed desilylation procedures, the latter being not useful for the deprotection of some silylated tertiary alcohols.
New Simple Polymeric Supports with Hydrazone Linkers for Solid-Phase Synthesis of Ketones and Primary Amines
Lazny, Ryszard,Nodzewska, Aneta,Wolosewicz, Karol
, p. 2858 - 2864 (2007/10/03)
The preparation of new solid supports with hydrazine anchoring groups and their application to solid-phase synthesis of ketones and primary amines are described. The supports were used for immobilization of ketones, 4-tert-butylcyclohexanone, pentan-3-one, acetone, N-methylpiperidone, N-benzylpiperidone, and tropinone in the form of their hydrazones. The polymer-supported hydrazones were subjected to deprotonation/alkylation procedure (LDA/RX) once or twice. The resulting alkylated products were cleaved off the solid support on treatment with trifluoroacetic acid in tetrahydrofuran providing α-alkylated or α,α′-bisalkylated ketones or were subjected to reductive cleavage with borane in tetrahydrofuran to give β-alkylated or β,β′-bisalkylated primary amines.
Cyclizing compounds. 3. Local anesthetic action of N (ω haloalkyl) N methylaminoaceto 2,6 xylidides
Ross,Sandberg,Akerman,Domeij,Stening,Svensson
, p. 787 - 790 (2007/10/06)
A series of N (ω chloroalkyl) N methylaminoaceto 2,6 xylidides which are able to cyclize to quaternary ammonium derivates was synthesized and examined for local anesthetic action. As reference compounds the corresponding series of N alkylamine derivates were synthesized and tested. In both series of compounds the duration of anesthesia was prolonged by increasing the size of the side chain. In the N alkylamine series an optimal effect was obtained for the N hexylamine derivate. The duration of anesthesia produced by the cyclizing compounds in the sciatic nerve test in vivo was somewhat shorter than that for the noncyclizing compounds. The observation that the N 4 chlorobutyl derivate produced a longer block than the 5 chloropentylamine in this test indicates that the quaternary compounds formed may contribute to the duration of anesthesia.