Process for preparing hexahydroazepine, piperidine and pyrrolidine derivatives
US4296029A · kind A · utility
Assignee
Inventors
Key dates
| Filing date | Jun 23, 1980 |
| Grant date | Oct 20, 1981 |
| Priority date | — |
| Expiry date | Jun 23, 2000 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07D227/08
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
Abstract
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.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.