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Building block capable of transferring a functional entity

  • US 20060166197A1
  • Filed: 03/14/2003
  • Published: 07/27/2006
  • Est. Priority Date: 03/15/2002
  • Status: Abandoned Application
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1. A building block of the general formula
Complementing Element—

  • Linker—

    Carrier—

    C—

    F-connecting group—

    Functional entity precursor capable of transferring a functional entity to a recipient reactive group, wherein Complementing Element is a group identifying the functional entity precursor, Linker is a chemical moiety comprising a Spacer and a S—

    C-connecting group, wherein the Spacer is a valence bond or a group distancing the functional entity precursor to be transferred from the complementing element and the S—

    C-connecting group connects the spacer with the Carrier, Carrier is selected among the groups embedded imagewherein the Linker attaches to the Carrier through Y and W═

    CH or N R2═

    H, -Halogen, —

    NO2, —

    CN, —

    C(Halogen)3, —

    C(O)R3, —

    C(O)NHR3, C(O)NR32, —

    NC(O)R3, —

    S(O)2NHR3, —

    S(O)2NR32, —

    S(O)2R3, —

    P(O)2—

    R3, —

    P(O)—

    R3, —

    S(O)—

    R3, P(O)—

    OR3, —

    S(O)—

    OR3, —

    N+R33, wherein p is an integer of 0 to 3, R3═

    H, C1-C6 alkyl, C1-C6 alkenyl, C1-C6 alkynyl, or aryl, and Halogen is F, Cl, Br, or I, Y=absent, C1-C6 Alkylene, C1-C6 Alkenylene, C1-C6 Alkynylene, Arylene, Heteroarylene, Carbonyl, or —

    SO2CH2—

    , C—

    F-connecting group is embedded imagewhere the carrier is connected to the left hand side of the formulae and X═

    —

    C—

    , —

    S—

    , —

    P—

    , —

    S(O)—

    or —

    P(O)—

    , V═

    O, S, NH, or N—

    C1-C6 alkyl, and Z=O, S, and Functional entity precursor is H or selected among the group consisting of a C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C4-C8 alkadienyl, C3-C7 cycloalkyl, C3-C7 cycloheteroalkyl, aryl, and heteroaryl, said group being substituted with 0-3 R4, 0-3 R5 and 0-3 R9, or selected among the group consisting of C1-C3 alkylene-NR42, C1-C3 alkylene-NR4C(O)R8, C1-C3 alkylene-NR4C(O)OR8, C1-C2 alkylene-O—

    NR42, C1-C2 alkylene-O—

    NR4C(O)R8, and C1-C2 alkylene-O—

    NR4C(O)OR8 substituted with 0-3 R9. where R4 is H or selected independently among the group consisting of C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C3-C7 cycloalkyl, C3-C7 cycloheteroalkyl, aryl, heteroaryl, said group being substituted with 0-3 R9 and R5 is selected independently from —

    N3, —

    CNO, —

    C(NOH)NH2, —

    NHOH, —

    NHNHR6, —

    C(O)R6, —

    SnR63, —

    B(OR6)2, —

    P(O)(OR6)2 or the group consisting of C2-C6 alkenyl, C2-C6 alkynyl, C4-C8 alkadienyl said group being substituted with 0-2 R7, where R6 is selected independently from H, C1-C6 alkyl, C3-C7 cycloalkyl, aryl or C1-C6 alkylene-aryl substituted with 0-5 halogen atoms selected from —

    F, —

    Cl, —

    Br, and —

    I; and

    R7 is independently selected from —

    NO2, —

    COOR6, —

    COR6, —

    CN, —

    OSiR63, —

    OR6 and —

    NR62. R8 is H. C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C3-C7 cycloalkyl, aryl or C1-C6 alkylene-aryl substituted with 0-3 substituents independently selected from —

    F, —

    Cl, —

    NO2, —

    R3, —

    OR3, —

    SiR33 R9 is ═

    O, —

    F, —

    Cl, —

    Br, —

    I, —

    CN, —

    NO2, —

    OR6, —

    NR62, —

    NR6—

    C(O)R8, —

    NR6—

    C(O)OR8, —

    SR6, —

    S(O)R6, —

    S(O)2R6, —

    COOR6, —

    C(O)NR62 and —

    S(O)2NR62.

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