Synthesis of 2(3H)‐benzoxazolinone derivatives as potential beta‐3‐adrenergic receptor ligands

Abstract

Beta‐3‐subtype‐adrenoceptors mediate lipolysis and in the search for potential beta‐3‐adrenergic receptor agonists for the treatment of obesity, we designed new arylethanolamines, structures B1 and B2, derived from 2(3H)‐benzoxazolinone. To obtain these target compounds as starting materials, various N‐benzyl‐[2(3H)‐benzoxazolinon‐6‐yl]ethylamines were used.

Synthesis of 2(3H)‐benzoxazolone and 2(3H)‐benzothiazolone derivatives as potential beta‐3‐adrenergic receptor ligands (part 2)

“…Hence, efforts are underway in our laboratory to synthesize novel, potent and selective beta-3-adrenergic receptor agonists. In a recent work [7] we describe the preparation of compound 3 ( Figure 2) which includes two 2(3H)-benzoxazolone heterocycles: the first one filling the place of the phenyl ring of the phenylethanolamine moiety, the second one bearing the acidic functionality of the arylalkyl group.…”