214360-51-7

Basic information

• Product Name: 4-SULFAMOYLPHENYLBORONIC ACID, PINACOL ESTER
• Synonyms: 4-SULFAMOYLPHENYLBORONIC ACID, PINACOL ESTER;BENZENESULFONAMIDE-4-BORONIC ACID PINACOL ESTER;4-(4,4,5,5-Tetramethyl-[1,3,2]dioxaborolan-2-yl)benzenesulfonamide;4-Boronobenzenesulfonamide,pinacol ester;Benzenesulfonamide-4-boronic acid pinacol ester ,98%;4-Sulphamoylbenzeneboronic acid, pinacol ester;4-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)benzenesulphonamide;3-hydroxy-2,3-dimethylbutan-2-yl hydrogen (4-sulfamoylphenyl)boronate
• CAS NO: 214360-51-7
• Molecular Formula: C₁₂H₁₈BNO₄S
• Molecular Weight: 283.15
• Product Categories: Aryl;Organoborons;Sulfonamide;Amines;Boron Derivatives;Intermediates;Intermediates & Fine Chemicals;Pharmaceuticals;Sulfur & Selenium Compounds
• Mol File: 214360-51-7.mol

Chemical Properties

• Boiling Point: 427.143 °C at 760 mmHg
• Flash Point: 212.129 °C
• Appearance: /
• Density: 1.242 g/cm³
• Vapor Pressure: 0mmHg at 25°C
• Refractive Index: 1.543
• Storage Temp.: under inert gas (nitrogen or Argon) at 2-8°C
• PKA: 10.00±0.10(Predicted)
• CAS DataBase Reference: 4-SULFAMOYLPHENYLBORONIC ACID, PINACOL ESTER(CAS DataBase Reference)
• NIST Chemistry Reference: 4-SULFAMOYLPHENYLBORONIC ACID, PINACOL ESTER(214360-51-7)
• EPA Substance Registry System: 4-SULFAMOYLPHENYLBORONIC ACID, PINACOL ESTER(214360-51-7)

Safety Data

• Hazardous Substances Data: 214360-51-7(Hazardous Substances Data)

Usage

Uses

4-SULFAMOYLPHENYLBORONIC ACID, PINACOL ESTER is used for preparation of Valdecoxib.

InChI:InChI=1/C12H18BNO4S/c1-11(2)12(3,4)18-13(17-11)9-5-7-10(8-6-9)19(14,15)16/h5-8H,1-4H3,(H2,14,15,16)

Upstream product

• 701-34-8 4-bromo-benzenesulfonic acid amide 
• 76-09-5 2,3-dimethyl-2,3-butane diol 
• 98-58-8 4-bromobenzenesulfonyl chloride 
• 63-74-1 sulfanilamide 
• 73183-34-3 bis(pinacol)diborane 

Downstream Products

• 477252-03-2 N-Cyclopropyl-1-[3-(4-sulfamoylphenyl)phenyl]-1,4-dihydro[1,8]naphthyridin-4-one-3-carboxamide 
• 1148110-23-9 4-[7-(4-piperidinyloxy)-6-isoquinolinyl]benzenesulfonamide 
• 1611000-62-4 4-(6-(4-(tert-butyl)phenyl)-8-(trifluoromethyl)imidazo[1,2-a]pyridin-3-yl)benzene sulfonamide 
• 1611000-33-9 4-(8-fluoro-6-(pyridin-3-yl)imidazo[1,2-a]pyridin-3-yl)benzene sulfonamide 
• 1366131-28-3 4-(2-amino-6-chloro-3-quinolinyl)benzenesulfonamide 
• 1332449-47-4 4-(6-(2,8-dimethyl-3,4-dihydro-1H-pyrido[4,3-b]indol-5(2H)-yl)pyridin-3-yl)benzenesulfonamide 
• 1332449-69-0 3'-(2,8-dimethyl-3,4-dihydro-1H-pyrido[4,3-b]indol-5(2H)-yl)biphenyl-4-sulfonamide 
• 1332449-79-2 2'-(2,8-dimethyl-3,4-dihydro-1H-pyrido[4,3-b]indol-5(2H)-yl)biphenyl-4-sulfonamide 
• 1246765-71-8 (R)-4-(1-(5-cyano-6-methylpyridin-2-yl)-5-cyclopentyl-4,5-dihydro-1H-pyrazol-3-yl)benzenesulfonamide 
• 1215006-89-5 C₁₆H₁₆N₄O₃S 
• 1152473-58-9 4-(2-(4-morpholinophenylamino)thieno[3,2-d]pyrimidin-7-yl)benzenesulfonamide 
• 1059170-80-7 4-(3-cyano-1H-pyrrolo[2,3-b]pyridin-5-yl)benzenesulfonamide 
• 1022981-65-2 4-(6-{[(3-fluorophenyl)methyl]amino}imidazo[1,2-b]pyridazin-3-yl)benzene-1-sulfonamide 
• 1071766-98-7 3'-(8-Methyl-4-oxo-7-trifluoromethyl-4,5-dihydro-3H-benzo[b][1,4]diazepin-2-yl)-biphenyl-4-sulfonic acid amide 

Relevant articles and documents

Rational Design, Optimization, and Biological Evaluation of Novel MEK4 Inhibitors against Pancreatic Adenocarcinoma

Growth, division, and development of healthy cells relies on efficient response to environmental survival cues. The conserved mitogen-activated protein kinase (MAPK) family of pathways interface extracellular stimuli to intracellular processes for this purpose. Within these pathways, the MEK family has been identified as a target of interest due to its clinical relevance. Particularly, MEK4 has drawn recent attention for its indications in pancreatic and prostate cancers. Here, we report two potent MEK4 inhibitors demonstrating significant reduction of phospho-JNK and antiproliferative properties against pancreatic cancer cell lines. Furthermore, molecular inhibition of MEK4 pathway activates the MEK1/2 pathway, with the combination of MEK1/2 and MEK4 inhibitors demonstrating synergistic effects against pancreatic cancer cells. Our inhibitors provided insight into the crosstalk between MAPK pathways and new tools for elucidating the roles of MEK4 in disease states, findings which will pave the way for better understanding of the MAPK pathways and development of additional probes.

NAPHTHYRIDINE DERIVATIVES AS PRC2 INHIBITORS

Disclosed are compounds of formula (I) or (II) that inhibit Polycomb Repressive Complex 2 (PRC2) activity. In particular, the present invention relates to compounds, pharmaceutical compositions and methods of use, such as methods of treating cancer using the compounds and pharmaceutical compositions of the present invention.

IMIDAZO[1,2-C]PYRIMIDINE DERIVATIVES AS PRC2 INHIBITORS FOR TREATING CANCER

Disclosed are compounds that inhibit Polycomb Repressive Complex 2 (PRC2) activity. In particular, disclosed are compounds of Formula (I) and pharmaceutical compositions thereof, and methods of using the compounds and pharmaceutical compositions in, for example, methods of treating cancer.

PRC2 INHIBITORS

The present invention relates to compounds that inhibit Polycomb Repressive Complex 2 (PRC2) activity. In particular, the present invention relates to compounds, pharmaceutical compositions and methods of use, such as methods of treating cancer using the compounds and pharmaceutical compositions of the present invention. (Formula (I))

Discovery and evaluation of 3,5-disubstituted indole derivatives as Pim kinase inhibitors

Pim kinases are promising therapeutic targets for the treatment of hematological cancers. A potent Pim kinase inhibitor 7f, derived from meridianin C, was further optimized by the replacement of 2-aminopyrimidine with substituted benzene. The optimization of the C-3 and C-5 positions of indole yielded compound 43 with improved cellular potency and high selectivity against a panel of 14 different kinases.

Chemical Compounds

The present invention relates to imidazopyridazine derivatives. More particularly, it relates to 4-(biphenyl-3-yl)-7H-imidazo[4,5-c]pyridazine derivatives of formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4 and R5 are as defined in the description. The imidazopyridazine derivatives of the present invention modulate the activity of the GABAA receptor. They are useful in the treatment of a number of conditions, including pain.

Syntheses of (4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)arenes through Pd-catalyzed borylation of arylbromides with the successive use of 2,2′-bis(1,3,2-benzodioxaborole) and pinacol

Syntheses of (4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)arenes through the Pd-catalyzed borylation of arylbromides with the successive use of 2,2′-bis(1,3,2-benzodioxaborole) and pinacol were investigated. PdCl 2(dppf) and AcOK in EtOH or DMSO successfully provided (4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)arenes. In particular, this method was more effective in the borylation of arylbromides bearing sulfonyl groups than the conventional Pd-catalyzed borylation using pinacolborane or bis(pinacolato)diboron.

Sandmeyer-type reaction to pinacol arylboronates in water phase: A green borylation process

Copper(I)-catalyzed cross-coupling reactions of aryl diazonium salts with bis(pinacolato)diboron can proceed smoothly in the water phase at room temperature to give the corresponding arylboronate esters in good to high yields. The Sandmeyer-type borylation not only provides direct access to arylboronates bearing halo and acidic substituents, but also achieves a green borylation process. Georg Thieme Verlag Stuttgart · New York.

SUBSTITUTED BIPHENYL DERIVATIVE

The present invention relates to a biaryl derivative or a pharmacologically acceptable salt thereof having an excellent collagen-synthesis inhibition activity. A biaryl derivative having a structure represented by the following General Formula (I) or a pharmacologically acceptable salt thereof: wherein R1 represents a C6-C10 aryl group which is substituted with one to three group(s) each independently selected from the group consisting of a group defined by formula R-L-, a di-(C1-C6 alkyl)amino group, a di-(C1-C6 alkyl)aminosulfonyl group, a hydroxyaminocarbonyl group, and a halogen atom, and so on; R represents a C1-C6 alkyl group, and so on; L represents a sulfonyl group, an aminosulfonyl group, or a sulfonylamino group, and so on; R2 represents a hydrogen atom, and so on; A represents a group defined by formula (II), (III), or (IV); R3 represents a C1-C6 alkyl group, and so on; and R4 represents a C1-C6 alkyl group, and so on.

New phenylpyridylpiperazine compounds

A compound selected from those of formula (I): [image] wherein: X represents a C(O) or SO2 group, R1 represents an aryl group or a group NR3R4 wherein R3 and R4 are as defined in the description, R2 represents an alkyl, (C3-C8)cycloalkyl or (C3-C8)cycloalkyl-(C1-C6)alkyl group, its isomers, and addition salts thereof, and medicinal products containing the same which are useful in treating conditions treatable by antagonists of type H3 central histamine receptors.