Process for the preparation of 2H-3-isoquinolones

Details Process for the preparation of 2H-3-isoquinolones Process for the preparation of 2H-3-isoquinolones

1973-05-31

1976-05-04

Gallagher, R.

Chemistry of carbon compounds

Miscellaneous organic carbon compounds

C-metal

260289D, C07D21732

Patent

active

039547710

ABSTRACT:
A process for the preparation of 2H-3-isoquinolones having the formula ##SPC1##
Wherein R.sub.1 and R.sub.2 are each hydrogen, halogen, lower alkyl, lower alkoxy, aryl, haloaryl, alkylaryl or alkoxyaryl; R.sub.3 and R.sub.4 are each hydrogen, lower alkyl, lower alkoxyalkyl, lower alkenyl, lower alkynyl, cycloalkyl, aryl, aralkyl, or halo-aralkyl, which comprises cyclizing an N-formyl-2-phenyl-acetamide of the formula ##SPC2##
Wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 have the same meaning as above, with a cyclodehydration agent. Said 2H-3-isoquinolones are useful as starting materials e.g. in the synthesis of 1,4-dihydro-1,4-etheno-isoquinolin-3(2H)-ones which are valuable chemotherapeutic agents in the treatment of disorders of the central nervous system, such as troubles of wakefulness, disorders of equilibrium and vertigo.

REFERENCES:
patent: 2759936 (1956-08-01), Skeeter
patent: 3457266 (1969-07-01), Gibas
Haworth, J. Chem. Soc. (1927) pp. 2281-2284.

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