Palladium catalyzed indolization
US5811551A · kind A · utility
Assignee
Inventors
Key dates
| Filing date | Aug 7, 1997 |
| Grant date | Sep 22, 1998 |
| Priority date | — |
| Expiry date | Aug 7, 2017 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07D491/10
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
Abstract
We have found that indoles of structural formula (III): ##STR1## can be cost-effectively synthesized in high yield by the palladium-catalyzed coupling/ring closure of a 2-halo- or 2-trifluoromethylsulfonyl-aniline and a cyclic ketone derivative. The process of the present invention is particularly useful to form indoles containing acid-labile substituents such as triazole, acetyl, ketal, cyano, and carbamate, or indoles having a good leaving group in the benzyl position. The advantages of the present process are that it does not require the use of triphenyl phosphine or tetrabutyl ammonium chloride or lithium chloride. By this invention, there is provided a process comprising the step of contacting a compound of Structure I with a compound of Structure II to form a compound of StructureIII: ##STR2##
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.