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Amino amides, peptides and peptidomimetics

  • US 6,946,542 B2
  • Filed: 04/01/2003
  • Issued: 09/20/2005
  • Est. Priority Date: 04/01/2002
  • Status: Expired due to Fees
First Claim
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1. A method for preparing a peptide, the method comprising:

  • providing an amino derivative of formula 6embedded image

    wherein;

    R1, R2 and R4 are independently selected from a group consisting of hydrogen, alkyl, allyl, alkenyl, aryl, heteroaryl, acyl, sulfonyl, amino, alkylamino, dialkylamino, acylamino, sulfonylamino, and alkoxy, provided that two or more of R1, and R2 R4 can be connected together forming one or more rings;

    R3 is alkyl, aryl, heteroaryl, allyl, alkenyl, alkynyl or allenyl; and

    Rw is hydrogen, alkyl, aryl, heteroaryl;

    converting the amino amide derivative of formula 6 to a compound of formula 7 embedded image

    wherein;

    Rw′

    is hydrogen, alkyl, aryl, heteroaryl;

    contacting the compound of formula 7 with an amine of formula 8 and an organoboron compound of formula 9 to form a reaction mixture embedded image

    wherein;

    R5 is alkyl, aryl, heteroaryl, allyl, alkenyl, alkynyl, or allenyl;

    Rc and Rd are independently selected from a group consisting of hydrogen, alkyl, allyl, benzyl, aryl, heteroaryl, acyl, sulfonyl, amino, acylamino, sulfonylamino, and alkoxy, provided that Rc and Rd can be joined together forming a ring; and

    X and Y are independently selected from a group consisting of hydroxy, alkoxy, aryloxy, amino, alkylamino, and dialkylamino, provided that X and Y can also be joined together forming a ring; and

    allowing the reaction mixture to react to form a peptide of formula 10embedded image

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