13070-01-4Relevant articles and documents
Ring Expansion of Thiolactams via Imide Intermediates: An Amino Acid Insertion Strategy
Shang, Jing,Thombare, Varsha J.,Charron, Carlie L.,Wille, Uta,Hutton, Craig A.
supporting information, p. 1620 - 1625 (2020/12/23)
The AgI-promoted reaction of thiolactams with N-Boc amino acids yields an N-(α-aminoacyl) lactam that can rearrange through an acyl transfer process. Boc-deprotection results in convergence to the ring-expanded adduct, thereby facilitating an overall insertion of an amino acid into the thioamide bond to generate medium-sized heterocycles. Application to the site-specific insertion of amino acids into cyclic peptides is demonstrated.
ASK1 INHIBITOR AND PREPARATION METHOD AND USE THEREOF
-
Paragraph 0183, (2020/01/02)
The present disclosure relates to a compound as shown in formula (II), a tautomer or a pharmaceutically acceptable salt thereof, and disclosed is the use thereof in preparing a drug for treating an ASK1-associated disease.
Ruthenium catalyzed synthesis of enaminones
Koduri, Naga Durgarao,Scott, Halee,Hileman, Bethany,Cox, Justin D.,Coffin, Michael,Glicksberg, Lindsay,Hussaini, Syed R.
supporting information; experimental part, p. 440 - 443 (2012/03/10)
The Grubbs first-generation catalyst has been found to be an effective catalyst for the synthesis of enaminones by coupling thioamides with α-diazodicarbonyl compounds. The reaction is successful in converting primary, secondary, and tertiary thioamides into their corresponding enaminones. The reaction is also suitable for the synthesis of chiral enaminones.