135525-70-1

Basic information

• Product Name: 3-[(1,3-benzoxazol-2-ylmethyl)amino]-5-ethyl-6-methylpyridin-2(1H)-one
• Synonyms: 2(1H)-Pyridinone, 3-[(2-benzoxazolylmethyl)amino]-5-ethyl-6-methyl-; 2-pyridinol, 3-[(2-benzoxazolylmethyl)amino]-5-ethyl-6-methyl-; 3-[(1,3-benzoxazol-2-ylmethyl)amino]-5-ethyl-6-methylpyridin-2-ol
• CAS NO: 135525-70-1
• Molecular Formula: C₁₆H₁₇N₃O₂
• Molecular Weight: 283.3251
• Mol File: 135525-70-1.mol

Chemical Properties

• Boiling Point: 509.9°C at 760 mmHg
• Flash Point: 262.2°C
• Density: 1.25g/cm³
• Vapor Pressure: 1.63E-10mmHg at 25°C
• Refractive Index: 1.632
• CAS DataBase Reference: 3-[(1,3-benzoxazol-2-ylmethyl)amino]-5-ethyl-6-methylpyridin-2(1H)-one(CAS DataBase Reference)
• NIST Chemistry Reference: 3-[(1,3-benzoxazol-2-ylmethyl)amino]-5-ethyl-6-methylpyridin-2(1H)-one(135525-70-1)
• EPA Substance Registry System: 3-[(1,3-benzoxazol-2-ylmethyl)amino]-5-ethyl-6-methylpyridin-2(1H)-one(135525-70-1)

Safety Data

• Hazardous Substances Data: 135525-70-1(Hazardous Substances Data)

Upstream product

• 143745-99-7 2-ethyl-3-oxobutanal sodium salt 
• 139393-81-0 5-ethyl-6-methyl-3-nitro-2(1H)-pyridinone 
• 205653-35-6 2-chloromethyl-5-bromo-4,7-dichlorobenzoxazole 
• 37721-85-0 4-bromo-3,6-dichloro-2-nitrophenol 
• 135397-32-9 3-amino-5-ethyl-6-methyl-pyridin-2(1H)-one 
• 205653-36-7 3-[(5-Bromo-4,7-dichloro-benzooxazol-2-ylmethyl)-amino]-5-ethyl-6-methyl-1H-pyridin-2-one 
• 41014-43-1 2-(chloromethyl)benzoxazole 

Relevant articles and documents

The synthesis of several tritiated non-nucleoside, HIV-1 reverse transcriptase inhibitors

The synthesis of three tritiated reverse transcriptase inhibitors is described herein. These compounds contained the benzoxazole ring linked to a 2-pyridinone ring by an aminomethylene group. The tritiated compounds were synthesized by hydrogenolysis of bromobenzoxazole precursors. The final tritiated compounds had specific activities ranging from 3-10 Cl/mmol.

Synthesis and Evaluation of 2-Pyridinone Derivatives as HIV-1-Specific Reverse Transcriptase Inhibitors. 2. Analogues of 3-Aminopyridin-2(1H)-one

A series of nonnulceoside 3-aminopyridin-2(1H)-one derivatives was synthesized and evaluated for HIV-1 RT inhibitory properties.Several analogs proved to be potent and highly selective antagonists with in vitro IC50 values as low as 19 nM in the enzyme assay using rC*dG as template*primer.Two compounds from this series, 3-amino>-5-ethyl-6-methylpyridin-2(1H)-one (34, L-697,639) and the corresponding 4,7-dichloro analogue (37, L-697,661) inhibited the spread of HIV-1 IIIb infection by 95percent in MT4 cell culture at concentrations of 25-50 nM and were selected for clinical trials as antiviral agents.

Synergism of HIV reverse transcriptase inhibitors

The combination of certain aminopyridones and anti-HIV nucleoside analogs has been found to synergistically inhibit HIV reverse transcriptase. This combination is useful in the prevention or treatment of infection by HIV and the treatment of AIDS, either as a combination of compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in further combination with other antivirals, anti-infectives, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.

Inhibitors of HIV reverse transcriptase

Novel pyridones inhibit HIV reverse transcriptase, and are useful in the prevention or treatment of infection by HIV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, anti-infectives, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.