John Wyeth Brother, Limited

Brian John Bushell

Alan C White

John Leheup Archibald

Robin G Shepherd

John Frederick Cavalla

John Lambert Jackson

Robert Anthony Newberry

2-Oxo-hexahydroazepine, -piperidine or pyrrolidines of formula ##STR1## wherein n is 2,3 or 4, R is hydrogen, lower alkyl, aryl(lower)alkyl, loweralkenylmethyl or cycloalkylmethyl, R.sup.1 is hydrogen or lower alkyl and R.sup.2 is hydrogen, lower alkyl or aryl(lower)alkyl are prepared by a novel process involving reaction of an anion of a lactam of formula ##STR2## where R.sup.3 is lower alkyl, aryl(lower)alkyl, trialkyl-, triaryl- or triarylalkyl-silyl with a benzyne of formula ##STR3## where R.sup.4 is lower alkyl, aryl(lower)alkyl or trialkyl-, triaryl- or triarylalkyl-silyl. The products are useful as intermediates for preparing pharmacologically active 2-unsubstituted -hexahydroazepine, -piperidine and pyrrolidine derivatives.

Process for preparing hexahydroazepine, piperidine and pyrrolidine

This invention relates to novel thiazole derivatives having the formula: ##SPC1## Wherein R represents an unsubstituted or substituted aryl radical; R.sup.1 and R.sup.2 independently represent hydrogen or lower alkyl; R.sup.3 represents hydrogen or lower alkyl; and --COZ represents an amide group; a carboxylic acid group or an ammonium or pharmaceutically acceptable alkali metal or alkaline earth metal salt thereof; or an ester group of formula --COOR.sup.4 wherein R.sup.4 represents an alkyl, aralkyl or aryl radical, which exhibit antilipemic activity.

Thiazole derivatives

The invention provides indolo[2,3-a]quinolizine derivatives which are active as hypotensive and anti-histamine agents. The invention also provides a pharmaceutical composition comprising an indolo[2,3-a]quinolizine derivative together with a pharmaceutical carrier.

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Southampton, United Kingdom

Brian John Bushell