Smithkline Beckman Corporation

Orum D Stringer

Joseph Weinstock

James W Wilson

Certain 2-amino-6-.omega.-aminoethylphenols and thiophenols are intermediates for preparing D.sub.2 -dopamine agonistic aminoethyl substituted 1,3-benzthiazol- and 1,3-benzoxazol-2(3H)-ones.

Intermediates for preparing 7-(2-aminoethyl)-1,3-benzthia- or oxa-

4-[2-(Dialkylamino)ethyl]-7-hydroxyisatins are prepared by internal condensation of an oxime followed by removal of protecting groups. The compounds are D.sub.2 -agonists and, thereby, have anti-hypertensive activity. A species of the group is 4-[2-(di-n-propylamino)ethyl]-4-hydroxyisatin.

4-[2-(dialkylamino)ethyl]-7-hydroxyisatins

Certain aminoethyl substituted 1,3-benzthiazol- and 1,3-benzoxazol-2(3H)-ones are D.sub.2 -dopamine agonists. These compounds are prepared by reacting an appropriate o-aminophenol or thiophenol with phosgene.

7-(2-Aminoethyl)-1,3-benzthia- or oxa-zol-2(3H)-ones

7-[2-Dialkylamino)ethyl]-4-hydroxy-1,3-benzimidazol-2-ones are prepared by oxidative cyclization of a urea, followed by removal of protective groups. The compounds are D.sub.2 -agonists and, thereby, have anti-hypertensive activity. A species of the group is 7[2-N,N-di-n-propylamino)ethyl]-4-hydroxyl-1,3-benzimidazol-2-one.

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Orum D Stringer