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ABSTRACT:
SUBMITTER: Kobayakawa T
PROVIDER: S-EPMC5767888 | biostudies-other | 2018 Jan
REPOSITORIES: biostudies-other
Kobayakawa Takuya T Matsuzaki Yudai Y Hozumi Kentaro K Nomura Wataru W Nomizu Motoyoshi M Tamamura Hirokazu H
ACS medicinal chemistry letters 20171227 1
The first rapid and efficient chemical synthesis of a cyclic Arg-Gly-Asp (RGD) peptide containing a chloroalkene dipeptide isostere (CADI) is reported. By a developed synthetic method, an <i>N</i>-<i>tert</i>-butylsulfonyl protected CADI was obtained utilizing diastereoselective allylic alkylation as a key reaction. This CADI was also transformed into an <i>N</i>-Fmoc protected CADI in a few steps. The CADI was used in Fmoc-based solid-phase peptide synthesis. The first synthesis of a CADI-conta ...[more]