Spiroindolones
AssigneeAmerican Home Products Corporation
InventorsChristopher A. Demerson, Leslie G. Humber
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Abstract
Herein is disclosed spiroindolone derivatives of the formula ##STR1## in which R.sup.1 is lower alkyl or carboxy(lower)alkyl, R.sup.2 is lower alkyl, R.sup.3 is lower alkyl or phenyl(lower)alkyl, and X is oxygen or CH.sub.2, or a therapeutically acceptable base addition salt thereof when R.sup.1 is carboxy(lower)alkyl, a process for their preparation, methods of using the derivatives and pharmaceutical compositions of the derivatives. The derivatives are useful for treating hypertension in a mammal.
Claims16
A compound of formula I ##STR8## in which R.sup.1 is lower alkyl or carboxy(lower)alkyl, R.sup.2 is lower alkyl, R.sup.3 is lower alkyl or phenyl(lower)alkyl, and X is oxygen or CH.sub.2, or a therapeutically acceptable base addition salt thereof when R.sup.1 is carboxy(lower)alkyl.
A process for preparing a compound of formula I ##STR9## in which R.sup.1 is lower alkyl or carboxy(lower)alkyl, R.sup.2 is lower alkyl, R.sup.3 is lower alkyl or phenyl(lower)alkyl, and X is oxygen or CH.sub.2, which comprises oxidizing a compound of formula II ##STR10## in which R.sup.2, R.sup.3 and X are as defined herein and R.sup.4 is lower alkyl or lower alkoxycarbonyl(lower)alkyl with sodium periodate to obtain, in the instance wherein R.sup.4 of the compound of formula II is lower alkyl, the corresponding compound of formula I in which R.sup.1 is lower alkyl, and R.sup.2, R.sup.3 and X are as defined herein, or in the instance wherein R.sup.4 of the compound of formula II is lower alkoxycarbonyl(lower)alkyl, the corresponding compound of formula III ##STR11## in which R.sup.2, R.sup.3 and X are as defined herein and R.sup.4 is lower alkoxycarbonyl(lower)alkyl, and hydrolyzing said compound of formula III under alkaline conditions to obtain the corresponding compound of formula I in which R.sup.1 is carboxy(lower)alkyl, and R.sup.2, R.sup.3 and X are as defined herein.
Dependencies are inferred from the claim text.