| 摘要 |
<p>Preparation of benzofuran-2-carboxamide compounds (I) comprises reacting carboxamide compounds (II) and benzaldehyde compounds (III) in the presence of a base. Preparation of benzofuran-2-carboxamide compounds of formula (I) comprises reacting carboxamide compounds of formula (R 1>R 2>N-C(=O)-CH(X)-C(=O)-O-R 8>) (II) and benzaldehyde compounds of formula (III) in the presence of a base. Either R 1>, R 2>3-7C cycloalkyl or 1-10C alkyl (both optionally substituted with A, where one or more CH 2 group of alkyl is replaced with O- or S-, CH=CH or C=C and one or more H atom of the alkyl group is replaced with Hal, OH, Ar, Het, 3-10C cycloalkyl, N(R 7>) 2CN, COOR 7>, CON(R 7>) 2, NR 7>COR 7>, NR 7>CON(R 7>) 2, NR 7>SO 2A or SO 2NR 7>) or H; or NR 1>R 2>3-7 membered unsaturated heterocyclic ring containing S(O) m group and/or 1 or 2 N, S and/or O (substituted with A, Hal, 3-10C cycloalkyl, OR 7>, N(R 7>) 2, CN, COOR 7>, CON(R 7>) 2, NR 7>COR 7> and/or carboxylic acid); A : 1-6C alkyl, where at least one CH 2 group is replaced with O-, S- or CH=CH, or at least one or more H is replaced with F; Ar : phenyl, biphenyl or naphthyl (all optionally substituted with Hal, A, OR 7>, N(R 7>) 2, NO 2, CN, COOR 7>, CON(R 7>) 2, NR 7>COR 7>, NR 7>CON(R 7>) 2, NR 7>SO 2A, COR 7>, SO 2NR 7> or S(O) mA); Het : aromatic mono- or bicyclic 5-10C heterocyclic residue containing 1-4 of N, S or O (substituted with 1-3 of Hal, A, -[C(R 7>) 2]O-Ar, -[C(R 7>) 2]O-cycloalkyl, OR 7>, N(R 7>) 2, NO 2, CN, COOR 7>, CON(R 7>) 2, NR 7>COA, NR 7>CON(R 7>) 2, NR 7>SO 2A, COR 7>, SO 2NR 7> or S(O) mA and/or carboxylic acid); Hal : F, Cl, Br or I; R 3>-R 5>H, A or 1-20C alkoxy; R 6>C-atom, Ar, aryloxy, COOR 7>, Hal, OH, CN, NO 2, N(R 7>) 2, NHCOR 7>, CH 2OH, CH 2OR 7> or CO(R 7>) 2, one of R 3>-R 6> is 4-benzyl-piperazinyl, 4-tert-butoxycarbonylpiperazin-1-yl, leaving group or piperazine compound of formula (1); R 7>H or A; Q : amino protecting group; X : Hal; R 8>A; n : 2-5; m : 1 or 2; and o : 0-4. [Image] [Image]</p> |
