Preparation of 6-chloro-5-fluoroindole via the use of palladium and copper-mediated heterocyclisations

Tetrahedron Letters

Volumn 43, Issue 42, 2002, Pages 7581-7583

  Adams, David R ^a   Duncton, Matthew A J ^a,b   Roffey, Jonathan R A ^a   Spencer, John ^a  

^a Vernalis PLC   (United Kingdom)

^b OSI Pharmaceuticals   (United Kingdom)

Author keywords

Catalysis; Coupling reactions; Indoles; Palladium and compounds

Indexed keywords

2 (6 CHLORO 5 FLUORO 1 INDOLYL) 1 METHYLETHYLAMINE; 6 CHLORO 5 FLUOROINDOLE; COPPER; INDOLE DERIVATIVE; PALLADIUM; SEROTONIN 2C AGONIST; UNCLASSIFIED DRUG;

ARTICLE; CHEMICAL PARAMETERS; CYCLIZATION; METHODOLOGY; SYNTHESIS;

EID: 0037078398     PISSN: 00404039     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0040-4039(02)01758-6     Document Type: Article

References (11)

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9. The palladium(0)-catalysed cross-coupling of a Grignard reagent with halobenzoic acids, halophenols and haloanilines has been disclosed previously. See Bumagin N.A., Luzikova E.V. J. Organomet. Chem. 532:1997;271.
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11. A large scale preparation of 6-chloro-5-fluoroindole using a modified Leimgruber-Batcho route will be detailed elsewhere.