852852-96-1Relevant academic research and scientific papers
One-pot synthesis of amides from carboxylic acids activated using thionyl chloride
Leggio,Belsito,De Luca,Di Gioia,Leotta,Romio,Siciliano,Liguori
, p. 34468 - 34475 (2016/06/13)
A one-pot synthesis of secondary and tertiary amides from carboxylic acids and amines by using SOCl2 has been developed. Also when sterically hindered amines were used as the starting materials, excellent yields of the corresponding amides were obtained. The amidation of N-protected α-amino acids with secondary amines proceeds effectively with good yields. The process works well also in the presence of acid sensitive groups and occurs with almost complete retention of stereochemical integrity of chiral substrates. This protocol could be extended to industrial large-scale production processes.
N-Nosyl-α-amino acids in solution phase peptide synthesis
Leggio, Antonella,Di Gioia, Maria Luisa,Perri, Francesca,Liguori, Angelo
, p. 8164 - 8173 (2008/02/08)
A highly efficient and practical synthesis of peptides in solution phase has been developed. The procedure is based on the use of p-nitrobenzenesulfonyl (nosyl) group for the protection of the amino function of α-amino acids. Every step of the procedure,
N-methylation of peptides on selected positions during the elongation of the peptide chain in solution phase
Di Gioia, M. Luisa,Leggio, Antonella,Liguori, Angelo
, p. 3892 - 3897 (2007/10/03)
An efficient and general solution-phase method for the site-specific N-methylation of peptides has been developed. This novel procedure involves synthesis of N-nosyl protected peptides and their subsequent N-methylation with diazomethane. Its efficiency w
