Facile synthesis of cyclopentapeptide, cyclo[Arg(NO2)-Gly-Asp(OBn)-D-Phe-Lys(Fmoc)], and its application in synthesis of integrin-targeting anticancer conjugate. Issue 21 (2nd November 2017)

• Record Type: Journal Article
• Authors: Ma, Da-You; Zhong, Tao; Wang, Long-Long; Liu, Li-Jun; Wang, Ying-Xiong; Liu, Su-You
• Is Part Of: Synthetic communications. Volume 47:Issue 21(2017)
• Page Start: 1985
• Page End: 1989
• Publication Date: 2017-11-02
• Subjects: Chlorambucil -- conjugate -- cR(NO2)GD(Bn)fK(Fmoc) -- cRGDfK -- integrin; Organic compounds -- Synthesis -- Periodicals; Chemistry, Organic; Synthesis; 547.205
• DOI: 10.1080/00397911.2017.1359626
• Languages: English
• ISSNs: 0039-7911

Abstract

ABSTRACT: An efficient approach for integrin-targeting c RGDfK conjugate synthesis has been developed using a new protected cyclopentapeptide, c R(NO2 )GD(Bn)fK(Fmoc), as the key intermediate. c R(NO2 )GD(Bn)fK(Fmoc) was conveniently prepared in high yield. The Fmoc group of this cyclopentapeptide was selectively removed under mild conditions which makes it an ideal intermediate for c RGDfK conjugate synthesis as was well demonstrated in this paper by the synthesis of c RGDfK chlorambucil conjugate. GRAPHICAL ABSTRACT: