Skip to main content
. 2021 Jul 20;64(15):10890–10899. doi: 10.1021/acs.jmedchem.1c00176

Scheme 1. Published Synthesis of Bicyclic Chimera 3.

Scheme 1

(i) Fmoc SPPS on CTC resin up to and including Fmoc-Dab (Alloc)-OH; (ii) Alloc/Allyl deprotection; (iii) ring closing on resin; (iv) Fmoc SPPS (with incorporation of Fmoc-Glu-OAllyl via side-chain carboxyl) up to and including final Fmoc-d-Dab(Boc)-OH, including removal of the final Fmoc group; (v) Allyl deprotection; (vi) mild acid cleavage from resin; (vii) solution-phase cyclization; (vii) TFA deprotection and RP-HPLC purification.