Trans-3-(4-oxo-4H-quinazolin-3-yl)-2-propenoic acid derivatives

Details Trans-3-(4-oxo-4H-quinazolin-3-yl)-2-propenoic acid derivatives Trans-3-(4-oxo-4H-quinazolin-3-yl)-2-propenoic acid derivatives

1980-04-23

1981-07-28

Coughlan, Jr., Paul M.

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

Organic compounds

Nitrogen attached directly or indirectly to the purine ring...

424251, 544288, C07D23990

Patent

active

042811279

ABSTRACT:
Trans-3-(4-oxo-4H-quinazolin-3-yl)-2-propenoic acid derivatives of the formula ##STR1## wherein R.sub.1 is hydrogen, lower alkyl, lower cycloalkyl, lower alkoxy, hydroxy, halo, lower alkykthio, lower alkylsulfinyl, lower alkylsulfonyl, di-(C.sub.1 -C.sub.7)alkyl-N(CH.sub.2).sub.n O-- or 2-hydroxyethoxy; R.sub.2 is hydrogen, lower alkyl or lower alkoxy; R.sub.3 is hydroxy, lower alkoxy, di-(C.sub.1 -C.sub.7)alkyl-N(CH.sub.2).sub.n O-- or di-(C.sub.1 -C.sub.7)alkyl-N(CH.sub.2).sub.n NH--; and n is 2 to 7; provided that at least one of R.sub.1 and R.sub.2 is other than hydrogen,
when R.sub.3 is hydroxy, a salt thereof with a pharmaceutically acceptable base, or when R.sub.3 is di-(C.sub.1 -C.sub.7)alkyl-N(CH.sub.2).sub.n O-- or di-(C.sub.1 -C.sub.7)alkyl-N(CH.sub.2).sub.n NH--, a salt thereof with a pharmaceutically acceptable acid, and a process for the preparation thereof, are described. The compounds of formula I are useful as agents in the prevention of allergic reactions.

REFERENCES:
Baker et al., J. of Org. Chem., vol. 17, pp. 35-51, (1952).
Yanaiet et al., Yakugaku Zasshi, (J. of Pharm. Soc. of Japan), vol. 86(1), pp. 69-71, (1966).

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