| 摘要 |
Preparation of a heterocyclic carboxamide compound of formula ArCONR<6>R<7> (I) comprises reacting a halogen compound of formula ArX (II) with carbon monoxide and an amine of formula R<6>-NH-R<7> (III), in the presence of palladium, a diphosphine of formula (IV) and a base. Ar = a 6-membered heterocyclic group of formula (a); A<1> = N or CR<1>; A<2> = N or CR<2>; A<3> = N or CR<3>; A<4> = N or CR<4>; A<5> = N or CR<5>; provided that at least one of A<1> - A<5> is N and that the ring does not contain two adjacent N atoms; R<1>-R<5> = H, 1-4C alkyl or aryl; and one of R<1> -R<5> may also be OR; R<6>, R<8> = H or 1-4C alkyl; R, R<7> = optionally substituted aromatic or heteroaromatic group; R<9>-R<12> = sec. or tert. 3-6C alkyl, 5-7C cycloalkyl or optionally substituted phenyl; Y = CH, NH, CHCH or O; n = 0 or 1; Q completes an optionally substituted, 5- or 6-membered saturated or aromatic carbo- or heterocyclic ring, (if aromatic, optionally complexed with a transition metal). Also claimed is a process for preparing (Ia) (as (I), where Ar is substituted by OR) in a two-step process comprising (1) forming (IIa) (as (II), where Ar is substituted by OR) from the corresponding compound with Cl, Br or I in place of OR, by reaction with ROH; and (2) reacting (IIa) as above. 3-Chloro-2-Ä3-(trifluoromethyl)phenoxyÜpyridine (IIb) is claimed as intermediate in the two-step process. |
