81316-56-5

Upstream product

• 13139-86-1 4-methoxyphenyl magnesium bromide 
• 67341-07-5 tert-butyl N-(2-hydroxy-2-phenylethyl)carbamate 
• 123-11-5 4-methoxy-benzaldehyde 
• 7568-93-6 2-Amino-1-phenylethanol 
• 96-09-3 styrene oxide 
• 2393-23-9 4-methoxy-benzylamine 
• 81316-49-6 2-(4-methoxyphenyl)-5-phenyl-4,5-dihydrooxazole 

Downstream Products

• 1257261-10-1 (+/-)-N-(4-methoxybenzyl)-N-(2-hydroxy-2-phenylethyl)-3-phenyl-glycidyl amide 
• 1174657-32-9 2-(N-tert-butoxycarbonyl-N-(p-methoxybenzyl)amino)-1-phenylethanol 
• 1345986-00-6 2-(tert-butoxycarbonyl(4-methoxybenzyl)amino)-1-phenylethyl 3-nitrobenzenesulfonate 
• 1345986-01-7 2-(tert-butoxycarbonyl(4-methoxybenzyl)amino)-1-phenylethyl 4-fluorobenzenesulfonate 
• 62888-60-2 7-methoxy-4-phenyl-1,2,3,4-tetrahydroisoquinoline 
• 1375744-73-2 3-benzoyl-1-benzyl-4-[(4-methoxyphenyl)methyl]-6-methylpiperazine-2,5-dione 
• 1375744-66-3 3-benzoyl-4-[(4-methoxyphenyl)methyl]-1-methylpiperazine-2,5-dione 
• 1375744-74-3 phenyl N-benzyl-N-[(1S)-1-{[(4-methoxyphenyl)methyl](2-oxo-2-phenethyl)carbamoyl}ethyl]carbamate 
• 1375744-88-9 4-nitrophenyl N-({[(4-methoxyphenyl)methyl](2-oxo-2-phenylethyl)carbamoyl}-methyl)-N-methylcarbamate 
• 1375744-67-4 phenyl N-({[(4-methoxyphenyl)methyl](2-oxo-2-phenethyl)carbamoyl}methyl)-N-methylcarbamate 
• 1375744-92-5 phenyl N-benzyl-N-[(1S)-1-[(2-hydroxy-2-phenethyl)[(4-methoxyphenyl)methyl]-carbamoyl]ethyl]carbamate 
• 1375744-86-7 phenyl N-{[(2-hydroxy-2-phenylethyl)[(4-methoxyphenyl)methyl]carbamoyl]-methyl}-N-methylcarbamate 
• 81316-57-6 4-phenyl-6-methoxy-1,2,3,4-tetrahydroisoquinoline 

Relevant academic research and scientific papers

Getting a Grip on the Undrugged: Targeting β-Catenin with Fragment-Based Methods

Aberrant WNT pathway activation, leading to nuclear accumulation of β-catenin, is a key oncogenic driver event. Mutations in the tumor suppressor gene APC lead to impaired proteasomal degradation of β-catenin and subsequent nuclear translocation. Restoring cellular degradation of β-catenin represents a potential therapeutic strategy. Here, we report the fragment-based discovery of a small molecule binder to β-catenin, including the structural elucidation of the binding mode by X-ray crystallography. The difficulty in drugging β-catenin was confirmed as the primary screening campaigns identified only few and very weak hits. Iterative virtual and NMR screening techniques were required to discover a compound with sufficient potency to be able to obtain an X-ray co-crystal structure. The binding site is located between armadillo repeats two and three, adjacent to the BCL9 and TCF4 binding sites. Genetic studies show that it is unlikely to be useful for the development of protein–protein interaction inhibitors but structural information and established assays provide a solid basis for a prospective optimization towards β-catenin proteolysis targeting chimeras (PROTACs) as alternative modality.

Synthesis, characterization and catalytic application of Bi2S3 microspheres for Suzuki-Miyaura cross-coupling reaction and chemoselective ring opening of epoxides

Bismuth sulfide (Bi2S3) prepared using L-cysteine, which served as both the sulfur source and the directing molecule for the formation of Bi2S3 as heterogeneous catalyst through solvothermal method. The prepared catalyst was examined by various techniques such as XRD, BET, FE-SEM, TEM, and TGA analysis. The results and analysis revealed that bismuth microspheres have better catalytic behavior for the preparation of biphenyl in water as a greenest solvent and for the ring opening of epoxides by nucleophiles including amines, alcohol, and thiol compared to pure Bi(NO3)3. 3H2O under solvent-free condition. Moreover, the novel catalyst could be recovered and reusedat least four times without loss of its catalytic activity.

SUMO INHIBITOR COMPOUNDS AND USES THEREOF

The present invention relates to compounds and compositions capable of acting as inhibitors of small ubiquitin-like modifier (SUMO) family of proteins. The compounds and compositions may be used in the treatment of cancer. There are disclosed, inter alia, methods of inhibiting an E1 enzyme, and compounds useful for inhibiting an E1 enzyme.

Highly regioselective ring-opening of epoxides with amines: A metal- A nd solvent-free protocol for the synthesis of β-amino alcohols

We herein report a metal- A nd solvent-free acetic acid-mediated ring-opening reaction of epoxides with amines. This process provides β-amino alcohols in high yields with excellent regioselectivity. Importantly, this epoxide ring-opening protocol can be used for the introduction of amines in natural products during late-stage transformations.

A Dieckmann cyclization route to piperazine-2,5-diones

Piperazine-2,5-diones are formed by Dieckmann cyclization (NaH, THF) of substructures of the type CH2-N(R)C(O)CH2N(R′) CO2Ph in which the terminal methylene (CH2) that is adjacent to nitrogen closes onto the carbonyl group of the phenyl carbamate unit at the other end of the chain. R and R′ are alkyl groups, and the terminal methylene is activated by a ketone carbonyl, a nitrile, an ester, or a phosphoryl group. The starting materials are assembled by standard acylation and oxidation processes, starting from a β-(alkylamino)alcohol, an (alkylamino)acetonitrile, an (alkylamino) ester, or an (alkylamino)methyl phosphonate.

Synthesis and 2D QSAR of O-sulphonated β-aminols derivatives as novel antifungal and antibacterial agents

Synthesis of a series of b-aminol derivatives using regioselective opening reaction catalyzed by SiO2 (60-120 mesh) and O-sulphonation in THF-KOH system, comprising tert-butoxycarbonyl at secondary nitrogen and evaluate for various stains of bacteria and fungi. SAR study of synthesized compound using backward regression analysis.

Synthesis of N-substituted Clausenamide analogues

A practical synthesis of N-substituted Clausenamide analogues, including (-) and (+) CM1, Piracetam analogue 1 and Nefiracetam analogue 2, have been developed.

Oxazolines. 2. 2-Substituted 2-Oxazolines as Synthons for N-(β-Hydroxyethyl)arylalkylamines, Intermediates in a Synthesis of 1,2,3,4-Tetrahydroisoquinolines and 2,3,4,5-Tetrahydro-1H-3-Benzazepines

2-(Arylalkyl)-2-oxazolines 4 (n = 1) and 2-aryl-2-oxazolines 4 (n = 0), the latter prepared in a novel reaction by cross-coupling aryl Grignard reagents with 2-(methylthio)-5-phenyl-2-oxazoline (10) and using palladium(II) chloride (14) as a catalyst, were reduced in a previously unreported reaction by diborane in refluxing THF to yield N-(β- hyroxyethyl)arylalkylamines 5 (n = 1,2).Amino alcohols 5 were cyclized to their respective heterocyclic derivatives 6 (n = 1,2) by treatment with H2SO4/TFA in refluxing methylene chloride.This paper disscuses how 2-substituted 2-oxazolines may be used to prepare1,2,3,4-tetrahydroisoquinolines 6 (n = 1) and 2,3,4,5-tetrahydro-1H-3-benzazepines 6 (n = 2) via amino alcohols 5.