Synthesis and antihypertensive activity of 4'-substituted spiro [4H-3, 1-benzoxazine-4, 4'-piperidin]-2 (1H)-ones

…, AP Roszkowski, AM Strosberg, S Baker…

Index: Clark; Caroon; Kluge; Repke; Roszkowski; Strosberg; Baker; Bitter; Okada Journal of Medicinal Chemistry, 1983 , vol. 26, # 5 p. 657 - 661

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Citation Number: 82

Abstract

A series of 4'-substituted spiro [4H-3, l-benzoxazine-4, 4'-piperidin]-2 (1H)-ones was prepared and evaluated for antihypertensive activity in the spontaneously hypertensive rat (SHR). The basic ring system was prepared in one step by condensation of dilithiated (tert- butoxycarbony1) aniline (3) with (tert-butoxycarbony1) piperidinone. Deprotection afforded 6, which was condensed with expoxides or alkyl halides to furnish the title compounds. ...