New aromatic or heteroaromatic Grignard reagents, useful as intermediates for e.g. drugs, preferably in carrier bound form for use in production of combinatorial libraries

摘要

Optionally carrier-bound aromatic or heteroaromatic Grignard reagents (I) are new. Grignard reagents of formula (I) are new. z = 0 or 1; X = halo or R2; A2-A5 = CH, CR2, N, P or CR3; A1 = O, S, NR6, CR2 or CR3 if z = 0; or CH, CR2, N, P or CR3 if z = 1; R1 = COOR2, CN, CONR3R'3 or halo; R2 = optionally substituted 1-10C alkyl, 3-10C cycloalkyl, (1-4C) alkylaryl, (1-4C) alkylheteroaryl or R5; R3 = H, optionally substituted 1-10C alkoxy, 3-10C cycloalkoxy, (1-4C) alkylaryloxy, (1-4C) alkylheteroaryloxy, R'3 or R5; R'3 = H, optionally substituted 1-10C alkyl, 3-10C cycloalkyl, (1-4C) alkylaryl, (1-4C) alkylheteroaryl or R5; R5 = solid carrier; R6 = optionally substituted 1-10C alkyl, 3-10C cycloalkyl, (1-4C) alkylaryl, (1-4C) alkylheteroaryl, optionally substituted (1-10C) alkylcarbonyl, (3-10C) cycloalkylcarbonyl, (1-4C) alkylarylcarbonyl, (1-4C) alkylheteroarylcarbonyl or arylsulfonyl; A1 + A5 = optionally substituted aromatic, saturated or partially unsaturated 5-8 membered ring, optionally containing one or more heteroatom(s) such as O, N, S or P; and provided that not more than 3 of A1-A5 are heteroatoms. AN Independent claim is included for the preparation of (I).