| 摘要 |
<p>Preparation of a heterocyclic carboxamide compound of formula ArCONR6R7 (I) comprises reacting a halogen compound of formula ArX (II) with carbon monoxide and an amine of formula R6-NH-R7 (III), in the presence of palladium, a diphosphine of formula (IV) and a base. Ar = a 6-membered heterocyclic group of formula (a); A1 = N or CR1; A2 = N or CR2; A3 = N or CR3; A4 = N or CR4; A5 = N or CR5; provided that at least one of A1 - A5 is N and that the ring does not contain two adjacent N atoms; R1-R5 = H, 1-4C alkyl or aryl; and one of R1 -R5 may also be OR; R6, R8 = H or 1-4C alkyl; R, R7 = optionally substituted aromatic or heteroaromatic group; R9-R12 = 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- [3-(trifluoromethyl) phenoxy]pyridine (IIb) is claimed as intermediate in the two-step process.</p> |
