1083168-94-8

Basic information

• Product Name: 2-Methoxy-3-nitro-5-(4,4,5,5-tetramethyl-[1,3,2] dioxaborolan-2-yl)-pyridine
• Synonyms: 2-Methoxy-3-nitro-5-(4,4,5,5-tetramethyl-[1,3,2] dioxaborolan-2-yl)-pyridine;2-Methoxy-3-nitropyridine-5-boronic acid pinacol ester, 96%;2-Methoxy-3-nitropyridin-5-ylboronic acid pinacol ester;2-methoxy-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-3-nitropyridine
• CAS NO: 1083168-94-8
• Molecular Formula: C₁₂H₁₇BN₂O₅
• Molecular Weight: 280.08478
• Mol File: 1083168-94-8.mol
• Article Data: 6

Chemical Properties

• Appearance: /
• Storage Temp.: under inert gas (nitrogen or Argon) at 2-8°C
• CAS DataBase Reference: 2-Methoxy-3-nitro-5-(4,4,5,5-tetramethyl-[1,3,2] dioxaborolan-2-yl)-pyridine(CAS DataBase Reference)
• NIST Chemistry Reference: 2-Methoxy-3-nitro-5-(4,4,5,5-tetramethyl-[1,3,2] dioxaborolan-2-yl)-pyridine(1083168-94-8)
• EPA Substance Registry System: 2-Methoxy-3-nitro-5-(4,4,5,5-tetramethyl-[1,3,2] dioxaborolan-2-yl)-pyridine(1083168-94-8)

Safety Data

• Hazardous Substances Data: 1083168-94-8(Hazardous Substances Data)

Usage

General Description

2-Methoxy-3-nitro-5-(4,4,5,5-tetramethyl-[1,3,2] dioxaborolan-2-yl)-pyridine is a chemical compound with the molecular formula C14H19BN2O4. It is a pyridine derivative with a methoxy group and a nitro group attached to the 2nd and 3rd carbons, respectively. Additionally, it contains a 4,4,5,5-tetramethyl-[1,3,2] dioxaborolan-2-yl group attached to the 5th carbon. 2-Methoxy-3-nitro-5-(4,4,5,5-tetramethyl-[1,3,2] dioxaborolan-2-yl)-pyridine is commonly used as a building block in organic synthesis and pharmaceutical research. Its unique structure and reactivity make it a valuable intermediate for the synthesis of various biologically active compounds and materials.

Upstream product

• 152684-30-5 5-bromo-2-methoxy-3-nitropyridine 
• 73183-34-3 bis(pinacol)diborane 

Downstream Products

• 1804518-04-4 2,5-dimethoxy-3-nitropyridine 
• 1083326-71-9 N-(2-methoxy-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-pyridin-3-yl)cyclopropanesulfonamide 
• 1551455-26-5 N-(2-methoxy-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)pyridin-3-yl)-2-fluorobenzenesulfonamide 
• 1552301-08-2 3-fluoro-N-(2-methoxy-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)pyridin-3-yl)benzenesulfonamide 
• 1550190-31-2 4-methoxy-N-(2-methoxy-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)pyridin-3-yl)benzenesulfonamide 
• 1550190-39-0 N-(2-methoxy-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)pyridin-3-yl)-4-(trifluoromethyl)benzenesulfonamide 
• 1366131-01-2 4-cyano-N-(2-methoxy-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)pyridin-3-yl)benzenesulfonamide 
• 1083326-67-3 N-(2-methoxy-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)pyridin-3-yl)benzenesulfonamide 
• 1848242-58-9 N-(5-{3-chloro-4-oxo-4H-pyrido[1,2-a]pyrimidin-7-yl}-2-methoxypyridin-3-yl)-2,4-difluorobenzenesulfonamide 

Relevant articles and documents

Synthesis and biological evaluation of 4-(piperid-3-yl)amino substituted 6-pyridylquinazolines as potent PI3Kδ inhibitors

PI3Kδ is an intriguing target for developing anti-cancer agent. In this study, a new series of 4-(piperid-3-yl)amino substituted 6-pyridylquinazoline derivatives were synthesized. After biological evaluation, compounds A5 and A8 were identified as potent PI3Kδ inhibitors, with IC50 values of 1.3 and 0.7 nM, respectively, which are equivalent to or better than idelalisib (IC50 = 1.2 nM). Further PI3K isoforms selectivity evaluation showed that compound A5 afforded excellent PI3Kδ selectivity over PI3Kα, PI3Kβ and PI3Kγ. A8 exhibited superior PI3Kδ/γ selectivity over PI3Kα and PI3Kβ. Moreover, compounds A5 and A8 selectively exhibited anti-proliferation against SU-DHL-6 in vitro with IC50 values of 0.16 and 0.12 μM. Western blot analysis indicated that A8 could attenuate the AKTS473 phosphorylation. Molecular docking study suggested that A8 formed three key H-bonds action with PI3Kδ, which may account for its potent inhibition of PI3Kδ. These findings indicate that 4-(piperid-3-yl)amino substituted 6-pyridylquinazoline derivatives were potent PI3Kδ inhibitors with distinctive PI3K-isoforms and anti-proliferation profiles.

FUSED HETEROARYLS AND THEIR USES

Provided are certain fused heteroaryls, compositions thereof and methods of use therefor.

1H-IMIDAZO[4,5-c]QUINOLINONE DERIVATIVES

The invention relates to the use of 1H-imidazo[4,5-c]quinolinone derivatives and salts thereof in the treatment of protein and/or lipid kinase dependent diseases and for the manufacture of pharmaceutical preparations for the treatment of said diseases; 1H-imidazo[4,5-c] quinolinone derivatives for use in the treatment of protein and/or lipid kinase dependent diseases; a method of treatment against said diseases, comprising administering the 1H- imidazo[4,5-c] quinofinone derivatives to a warm-blooded animal, especially a human; pharmaceutical preparations comprising an 1H-imidazo[4,5-c] quinolinone derivative, especially for the treatment of a protein and/or lipid kinase dependent disease; novel 1 H- imidazo[4,5-c] quinolinone derivatives; and a process for the preparation of the novel 1H- imidazo[4,5-c] quinolinone derivatives.