1073354-05-8

Basic information

• Product Name: 2-METHOXY-5-(4,4,5,5-TETRAMETHYL-1,3,2-DIOXABOROLAN-2-YL)NICOTINONITRILE
• Synonyms: 2-METHOXY-5-(4,4,5,5-TETRAMETHYL-1,3,2-DIOXABOROLAN-2-YL)NICOTINONITRILE;3-CYANO-2-METHOXYPYRIDINE-5-BORONIC ACID, PINACOL ESTER;3-Cyano-2-methoxypyridine-5-boronic acid,pinacol;5-Cyano-6-methoxypyridine-3-boronic acid pinacol ester
• CAS NO: 1073354-05-8
• Molecular Formula: C₁₃H₁₇BN₂O₃
• Molecular Weight: 260.09668
• Mol File: 1073354-05-8.mol
• Article Data: 6

Chemical Properties

• Appearance: /
• Storage Temp.: under inert gas (nitrogen or Argon) at 2-8°C
• CAS DataBase Reference: 2-METHOXY-5-(4,4,5,5-TETRAMETHYL-1,3,2-DIOXABOROLAN-2-YL)NICOTINONITRILE(CAS DataBase Reference)
• NIST Chemistry Reference: 2-METHOXY-5-(4,4,5,5-TETRAMETHYL-1,3,2-DIOXABOROLAN-2-YL)NICOTINONITRILE(1073354-05-8)
• EPA Substance Registry System: 2-METHOXY-5-(4,4,5,5-TETRAMETHYL-1,3,2-DIOXABOROLAN-2-YL)NICOTINONITRILE(1073354-05-8)

Safety Data

• Hazardous Substances Data: 1073354-05-8(Hazardous Substances Data)

Usage

General Description

2-Methoxy-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)nicotinonitrile is a highly specific type of chemical compound that plays a role in various specialized scientific applications. Its long, complex name signifies its unique structure and array of atoms. It contains elements such as carbon, hydrogen, nitrogen, oxygen, and boron organized in a specific arrangement. This chemical is often used in fine chemical and pharmaceutical contexts, such as in laboratory research or in the synthesis of other complex molecules. Though it might not be widely recognized outside of scientific circles, this compound contributes substantially to advancements in pharmaceuticals and other scientific fields. However, information regarding its properties, safety, and applications is specialized and likely not widely known outside of scientific and industrial contexts.

Upstream product

• 941294-54-8 5-bromo-2-methoxypyridine-3-carbonitrile 
• 73183-34-3 bis(pinacol)diborane 

Downstream Products

• 1431540-99-6 5-{4-[3-(4-acetyl-piperazine-1-carbonyl)-phenyl]-quinazolin-6-yl}-2-methoxy-nicotinonitrile 
• 1431541-32-0 2-methoxy-5-{4-[3-((R)-3-methylpiperazine-1-carbonyl)phenyl]quinazolin-6-yl}nicotinonitrile 
• 1443283-58-6 2-methoxy-5-[1-methyl-3-phenyl-4-(trifluoromethyl)-1H-pyrazolo[3,4-b]pyridin-6-yl]pyridine-3-carbonitrile 
• 1443776-44-0 2-methoxy-5-{4-[3-((R)-3-methyl-piperazine-1-carbonyl)-phenyl]-quinazolin yl}-nicotinonitrile 

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.

PYRAZOLOPYRIMIDINE DERIVATIVE AND USE THEREOF AS PI3K INHIBITOR

The present invention discloses a series of pyrazolopyrimidine derivatives and use thereof in preparing a medicament for treating a disease related to PI3K, and in particular, discloses a derivative compound of formula (I), a tautomer thereof or a pharmaceutically acceptable composition thereof.

QUINAZOLINE DERIVATIVES AS PI3K MODULATORS

The invention relates to substituted quinazoline derivative of the formula (I), wherein A, X1, X2, X3, X4 and R5 are as defined in the description. Such compounds are suitable for the treatment of a disorder or disease which is mediated by the activity of the PI3K enzymes.