182801-94-1

Upstream product

• 14320-38-8 cyclopent-3-enol 
• 175164-50-8 4-(tert-butyldiphenylsilyloxy)hepta-1,6-diene 
• 58479-61-1 tert-butylchlorodiphenylsilane 
• 2883-45-6 1, 6-heptadien-4-ol 

Downstream Products

• 817210-65-4 trans-3-(tert-butyldiphenylsilyloxy)-6-oxa-bicyclo[3.1.0]hexane 
• 819051-90-6 cis-3-(tert-butyldiphenylsilyloxy)-6-oxa-bicyclo[3.1.0]hexane 
• 439590-82-6 cis-3-{[tert-butyl(diphenyl)silyl]oxy}-6-[(4-methylphenyl)sulfonyl]-6-azabicyclo[3.1.0]hexane 
• 135827-32-6 (1S,4S)-4-(tert-Butyl-diphenyl-silanyloxy)-cyclopent-2-enol 
• 201054-55-9 (+)-(1R,4S)-1-hydroxy-4-[(tert-butoxycarbonyl)amino]-2-cyclopentene 
• 865302-27-8 (1R,4S)-4-(t-butyldiphenylsilanyloxy)cyclopent-2-enol 
• 657397-04-1 (-)-4-(N-tert-butoxycarbonylamino)cyclopentenone 
• 817210-67-6 [4-(tert-butyl-diphenyl-silanyloxy)-cyclopent-2-enyl]-carbamic acid tert-butyl ester 
• 817210-72-3 [4-(tert-butyl-diphenyl-silanyloxy)-2,3-dihydroxy-cyclopentyl]-carbamic acid tert-butyl ester 
• 817210-73-4 [(3aR,4S,6R,6aR)-6-(tert-Butyl-diphenyl-silanyloxy)-2,2-dimethyl-tetrahydro-cyclopenta[1,3]dioxol-4-yl]-carbamic acid tert-butyl ester 
• 817210-66-5 C₃₂H₃₈N₂O₇SSi 
• 817210-69-8 C₃₂H₃₈N₂O₇SSi 

Relevant academic research and scientific papers

Synthetic studies directed toward guianolides: an organoiron route to the 5,7,5 tricyclic ring system

A diastereoselective route to the 5,7,5-tricyclic core of the guianolides is presented. This route relies on Cope rearrangement of a divinylcyclopropane prepared by alkenyl Grignard addition to a (pentadienyl)iron(+1) cation, followed by oxidative decompl

Fit-for-purpose synthesis of dual leucine zipper kinase (DLK) inhibitor GNE-834

A practical fit-for-purpose synthesis of dual leucine zipper kinase (DLK) inhibitor GNE-834 (1) was developed. The key C[sbnd]C bond was constructed via a Suzuki–Miyaura cross-coupling of iodopyrazole 2 and pyridine boronic ester 3 to afford ketone 12. Su

Tetrahydrofuran-Based Transient Receptor Potential Ankyrin 1 (TRPA1) Antagonists: Ligand-Based Discovery, Activity in a Rodent Asthma Model, and Mechanism-of-Action via Cryogenic Electron Microscopy

Transient receptor potential ankyrin 1 (TRPA1) is a nonselective calcium-permeable ion channel highly expressed in the primary sensory neurons functioning as a polymodal sensor for exogenous and endogenous stimuli and has generated widespread interest as a target for inhibition due to its implication in neuropathic pain and respiratory disease. Herein, we describe the optimization of a series of potent, selective, and orally bioavailable TRPA1 small molecule antagonists, leading to the discovery of a novel tetrahydrofuran-based linker. Given the balance of physicochemical properties and strong in vivo target engagement in a rat AITC-induced pain assay, compound 20 was progressed into a guinea pig ovalbumin asthma model where it exhibited significant dose-dependent reduction of inflammatory response. Furthermore, the structure of the TRPA1 channel bound to compound 21 was determined via cryogenic electron microscopy to a resolution of 3 ?, revealing the binding site and mechanism of action for this class of antagonists.

DIHYDROPYRIMIDINE DERIVATIVES AND USES THEREOF IN THE TREATMENT OF HBV INFECTION OR OF HBV-INDUCED DISEASES

Provided are dihydropyrimidine derivatives which are useful in the treatment or prevention of HBV infection or of HBV-induced diseases, more particularly of HBV chronic infection or of diseases induced by HBV chronic infection, as well as pharmaceutical or medical applications thereof.

Growth Factor Receptor antagonists. Preparation method and application thereof

The invention relates to a small molecule antagonist for transforming growth factor β receptors, a method for preparing the small molecule antagonist, and application of the small molecule antagonist in preparation of drugs. The small molecule antagonist for transforming the growth factor β receptor has the application of treating and/or preventing various diseases mediated by ALK5, and has great clinical application potential.

OXADIAZOLE TRANSIENT RECEPTOR POTENTIAL CHANNEL INHIBITORS

The invention relates to compounds of formula I: (I) and pharmaceutically acceptable salts thereof. In addition, the present invention relates to methods of manufacturing and methods of using the compounds of formula I as well as pharmaceutical compositio

Boronic ester-linked macrocyclic lipopeptides as serine protease inhibitors targeting Escherichia coli type I signal peptidase

Type I signal peptidase, with its vital role in bacterial viability, is a promising but underexploited antibacterial drug target. In the light of steadily increasing rates of antimicrobial resistance, we have developed novel macrocyclic lipopeptides, linking P2 and P1′ by a boronic ester warhead, capable of inhibiting Escherichia coli type I signal peptidase (EcLepB) and exhibiting good antibacterial activity. Structural modifications of the macrocyclic ring, the peptide sequence and the lipophilic tail led us to 14 novel macrocyclic boronic esters. It could be shown that macrocyclization is well tolerated in terms of EcLepB inhibition and antibacterial activity. Among the synthesized macrocycles, potent enzyme inhibitors in the low nanomolar range (e.g. compound 42f, EcLepB IC50 = 29 nM) were identified also showing good antimicrobial activity (e.g. compound 42b, E. coli WT MIC = 16 μg/mL). The unique macrocyclic boronic esters described here were based on previously published linear lipopeptidic EcLepB inhibitors in an attempt to address cytotoxicity and hemolysis. We show herein that structural changes to the macrocyclic ring influence both the cytotoxicity and hemolytic activity suggesting that the P2 to P1’ linker provide means for optimizing off-target effects. However, for the present set of compounds we were not able to separate the antibacterial activity and cytotoxic effect.

1 -OXO-1,2-DIHYDROISOQUINOLIN-7-YL-(5-SUBSTITUTED-THIOPHEN-2-YL)-SULFONAMIDE COMPOUNDS, FORMULATIONS CONTAINING THOSE COMPOUNDS, AND THEIR USE AS AICARFT INHIBITORS IN THE TREATMENT OF CANCERS

1-Oxo-1,2-dihydroisoquinolin-7-yl-(5-substituted-thiophen-2-yl)-sulfonamide compounds, formulations containing those compounds, and their use as AICARFT inhibitors.

A general and scalable synthesis of aeruginosin marine natural products based on two strategic C(sp3)-H activation reactions

An efficient and scalable access to the aeruginosin family of marine natural products, which exhibit potent inhibitory activity against serine proteases, is reported. This synthesis was enabled by the strategic use of two different, recently implemented C(sp3)-H activation reactions. The first method led to the common 2-carboxy-6-hydroxyoctahydroindole (Choi) core of the target molecules on a large scale, whereas the second one provided rapid and divergent access to the various hydroxyphenyllactic (Hpla) subunits. This strategy allowed the synthesis of the aeruginosins 98B and 298A, with the latter being obtained in unprecedentedly large quantities.

PYRAZOLE DERIVATIVES AND USES THEREOF AS INHIBITORS OF DLK

The present invention provides for compounds of formula 0 and various embodiments thereof, and compositions comprising compounds of formula 0 and various embodiments thereof. In compounds of formula 0, the groups R1A, R1B, R1C, R1D, R2, R3, R4, R5 and R6 have the meaning as described herein. The present invention also provides for methods of using compounds of formula 0 and compositions comprising compounds of formula 0 as DLK inhibitors and for treating neurodegeneration diseases and disorders.