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MODIFIED NUCLEOSIDES OR NUCLEOTIDES

  • US 20170166961A1
  • Filed: 02/28/2017
  • Published: 06/15/2017
  • Est. Priority Date: 03/15/2013
  • Status: Active Grant
First Claim
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1. A modified nucleotide or nucleoside molecule comprising a ribose or deoxyribose sugar moiety having a removable 3′

  • -hydroxy protecting group forming a structure —

    O—

    CH(R)N3 covalently attached to the 3′

    -carbon atom, whereinR is selected from the group consisting of —

    C(R1)m(R2)n, —

    C(═

    O)OR3, —

    C(═

    O)NR4R5, —

    C(R6)2O(CH2)pNR7R8 and —

    C(R9)2O—

    Ph—

    C(═

    O)NR10R11;

    R1 is hydrogen, or optionally substituted alkyl;

    R2 is halogen;

    R3 is hydrogen or optionally substituted alkyl;

    each of R4 and R5 is independently selected from the group consisting of hydrogen, optionally substituted alkyl, optionally substituted aryl, optionally substituted heteroaryl, and optionally substituted aralkyl;

    each of R6 and R9 is selected from the group consisting of hydrogen, optionally substituted alkyl and halogen;

    each of R7, R8, R10 and R11 is independently selected from the group consisting of hydrogen, optionally substituted alkyl, optionally substituted aryl, optionally substituted heteroaryl, and optionally substituted aralkyl;

    m is an integer of 1 or 2;

    n is an integer of 1 or 2;

    provided that m+n is equal to 3; and

    p is an integer of 0 to 6.

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