121942-75-4

Upstream product

• 18162-48-6 tert-butyldimethylsilyl chloride 
• 591-27-5 m-Hydroxyaniline 
• 98525-64-5 tert-butyldimethyl-(3-nitrophenoxy)silane 
• 554-84-7 meta-nitrophenol 

Downstream Products

• 121942-76-5 2-methyl-3-(3'-dimethyl-tert-butylsilyloxyanilino)cyclohex-2-en-1-one 
• 265309-32-8 N-[3-(tert-butyl-dimethyl-silanyloxy)-phenyl]-2-cyano-acetamide 
• 591-27-5 m-Hydroxyaniline 
• 921608-26-6 {tert-butoxycarbonylmethyl-[3-(tert-butyl-dimethyl-silanyloxy)-phenyl]-amino}-acetic acid tert-butyl ester 
• 1119899-55-6 C₂₇H₂₈N₂O₃SSi 
• 1421689-94-2 4-(4-((tert-butyldimethylsilyl)oxy)but-1-yn-1-yl)-1-(3-((tert-butyldimethylsilyl)oxy)-phenyl)-3,3-dimethylazetidin-2-one 
• 1421689-35-1 2-(4-((tert-butyldimethylsilyl)oxy)but-1-yn-1-yl)-1-(3-((tert-butyldimethylsilyl)oxy)phenyl)-3,3-dimethylazetidine 
• 1421689-90-8 (E)-3-((tert-butyldimethylsilyl)oxy)-N-(5-((tert-butyldimethylsilyl)oxy)pent-2-yn-1-ylidene)aniline 
• 1584164-58-8 ethyl 2-({3-[(tert-butyldimethylsilyl)oxy]phenyl}amino)-2-(6-hydroxybenzo[d][1,3]dioxol-5-yl)acetate 

Relevant academic research and scientific papers

New non-symmetrical choline kinase inhibitors

Identification of novel and selective anticancer agents remains an important and challenging goal in pharmacological research. Choline kinase (ChoK) is the first enzyme in the CDP-choline pathway that synthesizes phosphatidylcholine (PC), the major phosph

Design of Trifluoroalkenyl Iodonium Salts for a Hypervalency-Aided Alkenylation–Cyclization Strategy: Metal-Free Construction of Aziridine Rings

The synthesis of fluorinated compounds and their use as pharmaceutical ingredients or synthetic building blocks have been in the focus of chemical and medicinal research. However, the efficient synthesis of trifluoromethylated nitrogen heterocycles is sometimes challenging. Herein, we disclose a simple aziridination process that relies on the use of amines and novel alkenyl iodonium reagents for the synthesis of strained, trifluoromethylated heterocycles. With the utilization of a newly designed and bench-stable but highly reactive hypervalent alkenyl iodonium species, these three-membered-ring heterocyclic compounds can be efficiently constructed from simple amines under mild conditions in the absence of transition-metal catalysts. The special reactivity of the new trifluoropropenyl synthon towards nucleophilic centers could be exploited in more general cyclization and alkenylation reactions in the future.

Convenient synthesis of deazaflavin cofactor FO and its activity in F420-dependent NADP reductase

F420 and FO are phenolic 5-deazaflavin cofactors that complement nicotinamide and flavin redox coenzymes in biochemical oxidoreductases and photocatalytic systems. Specifically, these 5-deazaflavins lack the single electron reactivity with O2 of riboflavin-derived coenzymes (FMN and FAD), and, in general, have a more negative redox potential than NAD(P)+. For example, F420-dependent NADP+ oxidoreductase (Fno) is critical to the conversion of CO2 to CH4 by methanogenic archaea, while FO functions as a light-harvesting agent in DNA repair. The preparation of these cofactors is an obstacle to their use in biochemical studies and biotechnology. Here, a convenient synthesis of FO was achieved by improving the redox stability of synthetic intermediates containing a polar, electron-rich aminophenol fragment. Improved yields and simplified purification techniques for FO are described. Additionally, Fno activity was restored with FO in the absence of F420. Investigating the FO-dependent NADP+/NADPH redox process by stopped-flow spectrophotometry, steady state kinetics were defined as having a Km of 4.00 ± 0.39 μM and a kcat of 5.27 ± 0.14 s-1. The preparation of FO should enable future biochemical studies and novel uses of F420 mimics.

Phosphorylated 3-heteroarylcoumarins and their use in fluorescence microscopy and nanoscopy

Photostable and bright fluorescent dyes with large Stokes shifts are widely used as markers in far-field optical microscopy, but the variety of useful dyes is limited. The present study introduces new 3-heteroaryl coumarins decorated with a primary phosph

Structure-activity relationships of natural quinone vegfrecine analogs with potent activity against VEGFR-1 and -2 tyrosine kinases

A series of analogs of vegfrecine, a natural quinone vascular endothelial growth factor receptor (VEGFR) tyrosine kinase inhibitor, was synthesized via oxidative amination of 2,5-dihydroxybenzamide with functionalized arylamine followed by ammonolysis and

SUBSTITUTED AMIDE COMPOUNDS USEFUL AS FARNESOID X RECEPTOR MODULATORS

Disclosed are compounds of Formula (I): or a stereoisomer, a tautomer, or a pharmaceutically acceptable salt or solvate thereof, wherein Q is: (i) halo, cyano, hydroxyl, NRxRx, C(O)OH, C(O)NH2, C1-6 alkyl substituted with zero to 6 R1a, or P(O)R1cR1c; or (ii) L R1; and A, X1, X2, X3, X4, Z1, Z2, R1, R1a, R1c, R2, R3a, R3b, Rx, L, a, b, and d are defined herein. Also disclosed are methods of using these compounds to modulate the activity of farnesoid X receptor (FXR); pharmaceutical compositions comprising these compounds; and methods of treating a disease, disorder, or condition associated with FXR dysregulation, such as pathological fibrosis, transplant rejection, cancer, osteoporosis, and inflammatory disorders, by using the compounds and pharmaceutical compositions.

COMPOUNDS AND METHODS TO ATTENUATE TUMOR PROGRESSION AND METASTASIS

This invention relates to certain compounds or pharmaceutically acceptable salts thereof, and for the use of the compounds to treat cancer. In another aspect, the disclosure relates to a pharmaceutical composition comprising a compound of Formula (1), For

Small-Molecule Covalent Modification of Conserved Cysteine Leads to Allosteric Inhibition of the TEAD?Yap Protein-Protein Interaction

The Hippo pathway coordinates extracellular signals onto the control of tissue homeostasis and organ size. Hippo signaling primarily regulates the ability of Yap1 to bind and co-activate TEA domain (TEAD) transcription factors. Yap1 tightly binds to TEAD4

Synthesis and in vitro evaluation of diverse heterocyclic diphenolic compounds as inhibitors of DYRK1A

Dual-specificity tyrosine phosphorylation-related kinase 1A (DYRK1A) is a dual-specificity protein kinase that catalyses phosphorylation and autophosphorylation. Higher DYRK1A expression correlates with cancer, in particular glioblastoma present within the brain. We report here the synthesis and biological evaluation of new heterocyclic diphenolic derivatives designed as novel DYRK1A inhibitors. The generation of these heterocycles such as benzimidazole, imidazole, naphthyridine, pyrazole-pyridines, bipyridine, and triazolopyrazines was made based on the structural modification of the lead DANDY and tested for their ability to inhibit DYRK1A. None of these derivatives showed significant DYRK1A inhibition but provide valuable knowledge around the importance of the 7-azaindole moiety. These data will be of use for developing further structure-activity relationship studies to improve the selective inhibition of DYRK1A.

BICYCLIC HETEROCYCLE DERIVATIVES AS BROMODOMAIN INHIBITORS

The invention relates to novel bicyclic heterocycle derivatives of formula (I) wherein Cy1,Cy2, R1,R2 and L have the meaning given in the specification, and pharmaceutically acceptable salts thereof. The compounds of formula (I) are usefulas bromodomain inhibitors in the treatment or prevention of diseases or disorders where bromodomain inhibition is desired.