2944-52-7

Upstream product

• 2078-54-8 2,6-diisopropylphenol 
• 1822-71-5 n-pentylsodium 
• 77-78-1 dimethyl sulfate 
• 74-88-4 methyl iodide 
• 186581-53-3 diazomethane 
• 74-83-9 methyl bromide 

Downstream Products

• 192766-86-2 bis(3,5-diisopropyl-4-methoxyphenyl)iodonium tetrafluoroborate 
• 2078-54-8 2,6-diisopropylphenol 
• 3883-87-2 4-methoxy-3,5-diisopropylaniline 
• 715-71-9 4-fluoro-2,6-diisopropylanisole 
• 221445-27-8 3,5-diisopropyl-4-methoxybenzaldehyde 
• 258516-89-1 fospropofol 
• 258516-82-4 2-(chloromethoxy)-1,3-diisopropylbenzene 
• 16221-07-1 3,5-Diisopropyl-4-methoxybenzylchlorid 
• 69129-70-0 3,5-Diisopropyl-4-methoxy-benzenesulfonyl chloride 

Relevant academic research and scientific papers

Synthesis method and application of propofol sodium and intermediate thereof

The method comprises an intermediate B and an intermediate C, and, the application of the phosphorus propofol sodium prepared by the synthesis method in an animal anesthetic sedative. The phosphorus propofol sodium synthesis method provided by the invention avoids the use of highly toxic reagent chlorobromomethane and is high in safety. The prepared propofol intermediate reaction condition is mild, the operation is simple and convenient, the quality yield is ＞ 97%, and the propofol prodrug synthesized by the synthetic method provided by the invention can generate the same clinical effect as the commercially available propofol emulsion injection.

Diastereo-, Enantio-, and anti-Selective Formation of Secondary Alcohol and Quaternary Carbon Stereocenters by Cu-Catalyzed Additions of B-Substituted Allyl Nucleophiles to Carbonyls

A general method for the synthesis of secondary homoallylic alcohols containing α-quaternary carbon stereogenic centers in high diastereo- and enantioselectivity (up to >20:1 dr and >99:1 er) is disclosed. Transformations employ readily accessible aldehydes, allylic diboronates, and a chiral copper catalyst and proceed by γ-addition of in situ generated enantioenriched boron-stabilized allylic copper nucleophiles. The catalytic protocol is general for a wide variety of aldehydes as well as a variety of 1,1-allylic diboronic esters. Hammett studies disclose that diastereoselectivity of the reaction is correlated to the electronic nature of the aldehyde, with dr increasing as aldehydes become more electron poor.

ALPHAvBETA1 INTEGRIN ANTAGONISTS

The present disclosure provides pharmaceutical agents, including those of the formula: (I) wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such pharmaceutical agents. Methods of using the pharmaceutical agents are also provided. The compounds may be used for the inhibition or antagonism of integrins ανβ1 and/or α5β1. In some embodiments, the compounds provided herein exhibit reduced inhibitory or antagonistic activity of integrins ανβ3, ανβ5, ανβ6, ανβ8, and/or αIIbβ3.

Microwave mediated protection of hindered phenols and alcohols

Hindered phenols and alcohols were protected as their corresponding ethers using different alkylating agents in presence of KOH/DMSO under microwave irradiation.

Nuclear receptor ligands and ligand binding domains

The present invention provides new methods, particularly computational methods, and compositions for the generation of nuclear receptor synthetic ligands based on the three dimensional structure of nuclear receptors, particularly the thyroid receptor (her

Nuclear receptor ligands and ligand binding domains

The present invention provides new methods, particularly computational methods, and compositions for the generation of nuclear receptor synthetic ligands based on the three dimensional structure of nuclear receptors, particularly the thyroid receptor (her

Propofol analogues. Synthesis, relationships between structure and affinity at GABA(A) receptor in rat brain, and differential electrophysiological profile at recombinant human GABA(A) receptors

A number of propofol (2,6-diisopropylphenol) congeners and derivatives were synthesized and their in a vitro capability to affect GABA(A) receptors determined by the inhibition of the specific [35S]-tert- butylbicyclophosphorothionate ([35S]TBPS) binding to rat whole brain membranes. Introduction of halogen (Cl, Br, and I) and benzoyl substituents in the para position of the phenyl group resulted in ligands with higher potency at inhibiting [35S]TBPS binding. A quantitative structure - affinity relationship (QSAR) study demonstrated that affinity is enhanced by increases in lipophilicity of the ligand whereas affinity is adversely affected by increases in size of the substituent para to the phenolic hydroxyl group. Consistent with the displacement of [35S]TBPS and with the activation of GABA(A) receptors, we demonstrate that ligands displaying high affinity (i.e., 2-4, and 8) are able to increase GABA-stimulated chloride currents in oocytes expressing human GABA(A) receptors and to directly activate chloride currents in an electrophysiological assay. Among them, compound 4 showed a rather peculiar profile in the electrophysiological examination with cloned α1β2γ2 GABA(A) receptors. Indeed, compared to propofol, it displayed a much greater efficacy at potentiating GABA-elicited chloride currents, but a much lower efficacy at producing a direct activation of the chloride channel in the absence of GABA. This behavior may give to compound 4 pharmacological properties that are more similar to anxiolytic and anticonvulsant drugs than to those of general anesthetics.

SYNTHESIS OF SOME FUNCTIONALIZED PHOSPHINOCARBOXYLIC ACIDS

Various functionalized phosphinocarboxylic acids have been prepared by a number of complementary methods.Reactions of relatively electron-poor secondary phosphides with electron-rich halocarboxylates in liquid ammonia give high yields of phosphinocarboxylates.The substitution reactionmay proceed by a classical SN2 mechanism or by an SN rad mechanism.Reduction of the carboxilate can be a deleterious side reaction in the preparation of phosphinoacetic acids.Several phosphinopropionic acids are prepared by the Michael adition of diphenylphosphine to unsaturated esters.A valuable method proved to be the reaction of dichlorophosphinoacetic ester with functionalized organometallic reagents. Key words: Phosphine; carboxylic acid; ligand; functionalized; synthesis; NMR data.

Enhancement of the Resonance Interaction of Out-of-Plane Methoxy Groups By Ortho Substituents in Crowded Anisoles

The 17O and 13C NMR chemical shifts of substituted anisoles provide evidence that the resonance interaction of methoxy groups which are perpendicular to the aromatic ring in crowded anisoles is influenced, to varying degrees, by ortho substituents.Enhance