Preparation of indole derivatives

Details Preparation of indole derivatives Preparation of indole derivatives

1976-06-01

1978-01-17

Love, Ethel G.

Chemistry of carbon compounds

Miscellaneous organic carbon compounds

C-metal

26032615, 26032616, C07D20904

Patent

active

040692302

ABSTRACT:
An improved process for preparing indole derivatives of the formula, ##STR1## wherein R.sub.1 and R.sub.2 each are hydrogen, halogen, C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkoxy, nitro, cyano or trifluoromethyl, or when taken together, form methylenedioxy; R.sub.3 is hydrogen, halogen, C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkoxy, nitro, cyano or dimethylamino; and R.sub.4 is hydrogen or halogen, which comprises cyclizing a compound of the formula, ##STR2## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are as defined above, with an acidic condensing agent.
The indole derivatives of the formula (I) mentioned above are useful as a key intermediate for the preparation of benzodiazepines, which are useful as tranquilizers, muscle relaxants and the like.

REFERENCES:
patent: 3632573 (1972-01-01), Yamamoto et al.
patent: 3790596 (1974-02-01), Suvorov et al.
Sundberg, The Chemistry of Indoles, pp. 148-158 and 208-213, 1970 Academic Press, N. Y. and London.

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