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. 2020 Dec 16;25(24):5966. doi: 10.3390/molecules25245966

Scheme 2.

Scheme 2

Synthesis of cyclo-[-isoAsp-Gly-Arg-(1R,2S)-β-ACPC-Val-] (10) via solid phase peptide synthesis of the linear counterpart 18 after cleavage from the resin, via in solution phase macrocyclization (19) and its full deprotection. a: 1% TFA in DCM, rt, 5 min for each cycle; b: HATU, DIPEA, DMF, rt, 30 min. c: TFA/Et3SiH/H2O, 95%/2.5%/2.5%, rt, 8 h. DIPEA = diisopropyl ethylamine, TFA = trifluoroacetic acid.