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DEPROTECTION METHOD

  • US 20160024143A1
  • Filed: 10/02/2015
  • Published: 01/28/2016
  • Est. Priority Date: 04/04/2013
  • Status: Active Grant
First Claim
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1. A method of deprotecting a sulfur-containing peptide containing at least one functional group selected from the group consisting of a carboxy group, an amino group, and a hydroxy group,wherein said peptide:

  • (1) is protected by a protecting group represented by formula (I);


    R1

    C(R2)(R3)-L1-  



    (I)wherein R1 is an aryl group optionally having one or more substituent(s), R2 and R3 are each, independently, a hydrogen atom or an aryl group optionally having one or more substituent(s), and L1 is a single bond, —

    O—

    CO—

    or —

    O—

    CH2

    ; and

    (2) contains at least one sulfur-containing amino acid residue selected from the group consisting of methionine, cysteine with protected sulfanyl group, and cysteine,wherein said method comprises subjecting said peptide to hydrogenation in the presence of a metal catalyst and a halogenated acetic acid.

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