1986•Journal of the Chemical Society Perkin Transactions 2Requires access

Nitrosation and nitrous acid-catalysed nitration of anisole and 2,6-dimethylanisole

Leslie R. Dix, Roy B. Moodie

Open publisher page 13 citations

Abstract

Rate–acidity profiles have been obtained for the nitrosation of anisole, 2,6-dimethylanisole (DMA), and 2,6-dimethylphenol (DMP) in aqueous sulphuric acid. The phenol is more reactive than the corresponding anisole, and DMA has a more shallow profile than anisole. A deuterium kinetic isotope effect (kH/kD) of 4.0 for [4-2H]anisole indicates that the product of nitrosation of anisole in 46.5% sulphuric acid (p-nitrosophenol) is formed by slow proton loss from the Wheland intermediate. Intense colours were associated with the nitrosation of these compounds when nitrous acid was in excess.The kinetics of nitrous acid-catalysed nitration of anisole were studied in 43.0 and 47.0% sulphuric acid; the product is p-nitrophenol. Nitrosation followed by oxidation by NV was the major pathway at these acidities. The other pathway has a kinetic form given by kC=k3[NIII][NV], consistent with a process where oxidation by NV is rate-limiting. Product studies show that p-nitrophenol is formed at lower acidities and o- and p-nitroanisole at higher acidities. A mechanism is suggested involving a radical cation species, which would predominate at higher acidities and account for the kC pathway at lower acidities.The nitrous acid-catalysed nitration of DMA gives 2,6-dimethyl-4-nitroanisole in higher yield as the acidity increases.

About this research paper

What this paper is about

Rate–acidity profiles have been obtained for the nitrosation of anisole, 2,6-dimethylanisole (DMA), and 2,6-dimethylphenol (DMP) in aqueous sulphuric acid. The phenol is more reactive than the corresponding anisole, and DMA has a more shallow profile than anisole. A deuterium kinetic isotope effect (kH/kD) of 4.0 for [4-2H]anisole indicates that the product of nitrosation of anisole in 46.5% sulphuric acid (p-nitrosophenol) is formed by slow proton loss from the Wheland intermediate. Intense colours were associated with the nitrosation of these compounds when nitrous acid was in excess.The kinetics of nitrous acid-catalysed nitration of anisole were studied in 43.0 and 47.0% sulphuric acid; the product is p-nitrophenol. Nitrosation followed by oxidation by NV was the major pathway at these acidities. The other pathway has a kinetic form given by kC=k3[NIII][NV], consistent with a process where oxidation by NV is rate-limiting. Product studies show that p-nitrophenol is formed at lower acidities and o- and p-nitroanisole at higher acidities. A mechanism is suggested involving a radical cation species, which would predominate at higher acidities and account for the kC pathway at lower acidities.The nitrous acid-catalysed nitration of DMA gives 2,6-dimethyl-4-nitroanisole in higher yield as the acidity increases.

Why it matters

OpenAlex reports 13 citations for this work. Citation counts describe recorded attention and do not establish research quality.

Key contribution

A contribution statement is not available in the OpenAlex record.

Method / approach

Method details are not available in the OpenAlex metadata.

Main findings

Findings are not separately available in the OpenAlex metadata.

Limitations

Limitations are not available in the OpenAlex metadata.

Applications

Application details are not available in the OpenAlex metadata.

Available abstract

Rate–acidity profiles have been obtained for the nitrosation of anisole, 2,6-dimethylanisole (DMA), and 2,6-dimethylphenol (DMP) in aqueous sulphuric acid. The phenol is more reactive than the corresponding anisole, and DMA has a more shallow profile than anisole. A deuterium kinetic isotope effect (kH/kD) of 4.0 for [4-2H]anisole indicates that the product of nitrosation of anisole in 46.5% sulphuric acid (p-nitrosophenol) is formed by slow proton loss from the Wheland intermediate. Intense colours were associated with the nitrosation of these compounds when nitrous acid was in excess.The kinetics of nitrous acid-catalysed nitration of anisole were studied in 43.0 and 47.0% sulphuric acid; the product is p-nitrophenol. Nitrosation followed by oxidation by NV was the major pathway at these acidities. The other pathway has a kinetic form given by kC=k3[NIII][NV], consistent with a process where oxidation by NV is rate-limiting. Product studies show that p-nitrophenol is formed at lower acidities and o- and p-nitroanisole at higher acidities. A mechanism is suggested involving a radical cation species, which would predominate at higher acidities and account for the kC pathway at lower acidities.The nitrous acid-catalysed nitration of DMA gives 2,6-dimethyl-4-nitroanisole in higher yield as the acidity increases.

Key concepts: Anisole, Nitrosation, Chemistry, Nitration, Phenol, Nitrous acid, Kinetic isotope effect, Medicinal chemistry

Related papers

Back to paper searchBrowse research topicsOriginal source
Nitrosation and nitrous acid-catalysed nitration of anisole and 2,6-dimethylanisole — Research Paper | ScholarLens