A highly chemoselective thioglycoconjugation method of iodoaryl aminoacids, small peptides and complex unprotected polypeptides is reported.

No abstract

A general strategy is introduced for the efficient synthetic access of disulfide linked artificial macrocycles via a Ugi four-component reaction (U4CR) followed by oxidative cyclization. The double-mercapto input is proposed for use in the Ugi reaction, thereby yielding all six topologically possible combinations. The protocol is convergent and short and enables the production of novel disulfide peptidomimetics in a highly general fashion.

The review provides a broad overview of amino acid chlorides in peptide chemistry, classified into different sections comprising reagents, N-protected amino acid chlorides (preparation and properties), coupling employing various protocols and applications in difficult and hindered couplings. The recent developments include their applications in synthesis of various amino acid derivatives, peptidomimetics, heterocycles and biologically active molecules.