Journal
ORGANIC LETTERS
Volume 16, Issue 20, Pages 5434-5437Publisher
AMER CHEMICAL SOC
DOI: 10.1021/ol5026684
Keywords
-
Categories
Funding
- National Institutes of Health [R21CA167215]
- Anna Valentine Cancer Fund (FIG award)
- NIH through the Moffitt Cancer Center [P30CA076292]
Ask authors/readers for more resources
The design and solid-phase synthesis of tetrahydropyridazine-3,6-dione (Tpd) peptidomimetics derived from backbone-aminated peptides is reported. The described protocol features the synthesis of chiral a-hydrazino acids suitable for chemoselective incorporation into growing peptide chains. Acid-catalyzed cyclization to form the Tpd ring during cleavage affords the target peptidomimetics in good yield and purity. The scope of Tpd incorporation is demonstrated through the synthesis of constrained peptides featuring nucleophilic/electrophilic side chains and sterically encumbered a-substituted hydrazino acid residues.
Authors
I am an author on this paper
Click your name to claim this paper and add it to your profile.
Reviews
Recommended
No Data Available