Process for the preparation of 4-quinolinones

Details Process for the preparation of 4-quinolinones Process for the preparation of 4-quinolinones

1984-09-20

1986-04-29

Daus, Donald G.

Organic compounds -- part of the class 532-570 series

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

260544R, 260544C, 544 97, C07D21522

Patent

active

045858675

ABSTRACT:
1,2,3,4-Tetrahydro-4-quinolinones of the formula ##STR1## are prepared from a 3-anilinopropionic acid of general for formula ##STR2## which is treated successively with phosgene, with a base or by heating, and then with a Lewis acid or a strong acid. In the formulae (I) and (II), R denotes a hydrogen atom, a halogen atom, an alkyl radical (1 to 4 carbon atoms) or an alkoxy radical (1 to 4 carbon atoms), and R.sub.1 denotes a hydrogen atom or any alkyl radical (1 to 4 carbon atoms). The compounds of formula I are useful as intermediates in the production of known drugs.

REFERENCES:
Organic Chemistry--Morrison and Boyd, 3rd Edition, pp. 665 and 669.
Hashimoto, Chem. Abstracts 86:190461x.
Johnson, J. Amer. Chem. Soc. 71, pp. 1901-1905 (1949).
Wasserman, J. Org. Chem. 27, pp. 35-39 (1961).

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