New Grignard compounds useful for production of substance libraries and in chemical syntheses

    公开(公告)号:DE19836408A1

    公开(公告)日:2000-02-24

    申请号:DE19836408

    申请日:1998-08-12

    Applicant: BASF AG

    Abstract: Grignard compounds (I) containing functional reactive substituents are new. Aromatic Grignard compounds (I) are new: z = 0 or 1; X = halo or R ; A, B, D and E = CH; CR ; N; P; or CR ; F = O, S, NR , CR or CR when z = 0 and CH, CR , N, P or CR when z = 1; or two adjacent symbols A-F form an optionally substituted aromatic, saturated or partly unsaturated 5-8 membered ring containing 1 or more hetero atoms, e.g. O, N, S or P; R = COOR ; CN; CONR R '; or halo; R = 1-10C alkyl, 3-10C cycloalkyl, 1-4C alkylaryl or 1-4C alkylheteroaryl (each optionally substituted) or R ; R = H; 1-10C alkyl, 3-10C cycloalkyl, 1-4C alkylaryl or 1-4C alkylheteroaryl (each optionally substituted); R '; or R ; R ' = H; 1-10C alkyl, 3-10C cycloalkyl, 1-4C alkylaryl or 1-4C alkylheteroaryl (each optionally substituted); or R ; R = 1-10C alkyl, 3-10C cycloalkyl, 1-4C alkylaryl or 1-4C alkylheteroaryl (each optionally substituted); or halo; R = solid carrier; R = 1-10C alkyl, 3-10C cycloalkyl, 1-4C alkylaryl or 1-4C alkylheteroaryl (each optionally substituted and optionally bonded via carbonyl); or -SO2-aryl; Not more than three of the variables A-F are heteroatoms. An Independent claim is also included for the preparation of compounds (I).

    New Grignard compounds useful for production of substance libraries and in chemical syntheses

    公开(公告)号:DE19816414A1

    公开(公告)日:1999-10-21

    申请号:DE19816414

    申请日:1998-04-14

    Applicant: BASF AG

    Abstract: Grignard compounds (I) containing functional reactive substituents are new. Aromatic Grignard compounds (I) are new: z = 0 or 1; X = halo or R ; A, B, D and E = CH; CR ; N; P; or CR ; F = O, S, NR , CR or CR when z = 0 and CH, CR , N, P or CR when z = 1; or two adjacent symbols A-F form an optionally substituted aromatic, saturated or partly unsaturated 5-8 membered ring containing 1 or more hetero atoms, e.g. O, N, S or P; R = COOR ; CN; CONR R '; or halo; R = 1-10C alkyl, 3-10C cycloalkyl, 1-4C alkylaryl or 1-4C alkylheteroaryl (each optionally substituted) or R ; R = H; 1-10C alkyl, 3-10C cycloalkyl, 1-4C alkylaryl or 1-4C alkylheteroaryl (each optionally substituted); R '; or R ; R ' = H; 1-10C alkyl, 3-10C cycloalkyl, 1-4C alkylaryl or 1-4C alkylheteroaryl (each optionally substituted); or R ; R = 1-10C alkyl, 3-10C cycloalkyl, 1-4C alkylaryl or 1-4C alkylheteroaryl (each optionally substituted); or halo; R = solid carrier; R = 1-10C alkyl, 3-10C cycloalkyl, 1-4C alkylaryl or 1-4C alkylheteroaryl (each optionally substituted and optionally bonded via carbonyl); or -SO2-aryl; Not more than three of the variables A-F are heteroatoms. An Independent claim is also included for the preparation of compounds (I).

    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

    公开(公告)号:DE19815078A1

    公开(公告)日:1999-10-07

    申请号:DE19815078

    申请日:1998-04-06

    Applicant: BASF AG

    Abstract: 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).

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