Process for the preparation of indolothiopyrones and indolylthio

Details Process for the preparation of indolothiopyrones and indolylthio Process for the preparation of indolothiopyrones and indolylthio

1976-05-10

1978-05-30

Daus, Donald G.

Chemistry of carbon compounds

Miscellaneous organic carbon compounds

C-metal

26029357, 26032612R, 26032628, 424274, 544142, C07D51304, A61K 3140, C07D49504

Patent

active

040923282

ABSTRACT:
This invention relates to novel indolothiopyrones having the formula: ##STR1## wherein R.sub.1 is hydrogen, lower alkyl or aryl; R.sub.2 is hydrogen or halogen; and R.sub.7 is hydrogen, lower alkyl, lower alkenyl, lower alkynyl, nitro-substituted-aryl, or .omega.-substituted lower alkyl wherein the substituent is: ##STR2## wherein R.sub.4 and R.sub.5 each represent hydrogen, lower alkyl, or together with the nitrogen atom, form a heterocyclic ring; and R.sub.6 is lower alkoxy or amino, and novel intermediates used in their preparation. The indolothiopyrones are prepared by reacting a 3-mercaptoindole with sodium propiolate or a substituted sodium propiolate followed by acidification to obtain an intermediate acid; the intermediate acid cyclizes in the presence of an acid catalyst to obtain the indolothiopyrone structure which may be additionally subjected to halogenation, alkylation or hydrolysis to obtain derivatives having the various substituent groups disclosed. The compounds of this invention are useful in the treatment of angina pectoris and conditions benefiting from the depression of the central nervous system.

REFERENCES:
patent: 3519648 (1970-07-01), Protiva et al.
patent: 3971806 (1976-07-01), Brown
patent: 4032537 (1977-06-01), Brown
Noller; Chem. of Org. Compounds; pp. 304; 611 (1965).

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