Van Lysebetten, Dorien; Felissati, Stefania; Antonatou, Eirini; Carrette, Lieselot L. G.; Espeel, Pieter; Focquet, Evelien; Du Prez, Filip E.; Madder, Annemieke published an article in 2018, the title of the article was A thiolactone strategy for straight-forward synthesis of disulfide-linked side-chain-to-tail cyclic peptides featuring an N-terminal modification handle.Name: 3-Aminodihydrothiophen-2(3H)-one hydrochloride And the article contains the following content:
The development of straight-forward and versatile peptide cyclization methods is highly desired to meet the demand for more stable peptide-based drugs. Herein, a new method for the synthesis of side-chain-to-tail cyclic peptides with the simultaneous introduction of an N-terminal handle, based on the introduction of an N-terminal thiolactone building block, is described. A primary amine liberates a homocysteine analog from the thiolactone building block, which further enables cyclization of the peptide through disulfide-bond formation with a C-terminal cysteamine. Postcyclisation modification can be achieved by using small bifunctional amines. Alternatively, the synthesis of lipopeptides is demonstrated through direct thiolactone opening with long-chain alkyl amines. The experimental process involved the reaction of 3-Aminodihydrothiophen-2(3H)-one hydrochloride(cas: 6038-19-3).Name: 3-Aminodihydrothiophen-2(3H)-one hydrochloride
The Article related to cyclic peptide synthesis disulfide thiolactone strategy, solid phase peptide synthesis cyclization aminolysis, lipopeptide synthesis thiolactone ring opening aminolysis, cyclisation, lactones, peptides, sulfur, synthesis design and other aspects.Name: 3-Aminodihydrothiophen-2(3H)-one hydrochloride
Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics