Vilsmeier–Haack reaction

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Template:Short description Template:Use dmy dates Template:Reactionbox The Vilsmeier–Haack reaction (also called the Vilsmeier reaction) is the chemical reaction of a substituted formamide (1) with phosphorus oxychloride and an electron-rich arene (3) to produce an aryl aldehyde or ketone (5):

Template:Awrap HArZ + POCl3 + H2O → RC(=O)ArZ + Template:Awrap HCl + H3PO4

The reaction is named after Anton Vilsmeier and Template:Interlanguage link.[1][2][3]

For example, benzanilide and dimethylaniline react with phosphorus oxychloride to produce an unsymmetrical diaryl ketone.[4] Similarly, anthracene is formylated at the 9-position.[5] The reaction of anthracene with N-methylformanilide, also using phosphorus oxychloride, gives 9-anthracenecarboxaldehyde:

File:Vilsmeier reaction example2.svg
N-Methylformanilide and anthracene and phosphorus oxychloride

In general, the electron-rich arene (3) must be much more active than benzene for the reaction to proceed; phenols or anilines are good substrates.[6]

Reaction mechanism

The reaction of a substituted amide with phosphorus oxychloride gives a substituted chloroiminium ion (2), also called the Vilsmeier reagent. The initial product is an iminium ion (4b), which is hydrolyzed to the corresponding ketone or aldehyde during workup.[7]

File:Vilsmeier Haack Reaction Scheme.png
The Vilsmeier–Haack reaction

See also

Further reading

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References

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