2754-02-1Relevant articles and documents
Phenysilane and Silicon Tetraacetate: Versatile Promotors for Amide Synthesis
Morisset, Eléonore,Chardon, Aurélien,Rouden, Jacques,Blanchet, Jér?me
supporting information, p. 388 - 392 (2020/01/24)
Phenylsilane was reevaluated as a useful coupling reagent for amide synthesis. At room temperature, a wide range of amides and peptides were obtained in good to excellent yields (up to 99 %). For the first time, Weinreb amides synthesis mediated by a hydrosilane were also documented. Comparative experiments with various acetoxysilanes suggested the involvement of a phenyl-triacyloxysilane. From this mechanistic study, silicon tetraacetate was shown as an efficient amine acylating agent.
Synthesis and biological evaluation of a novel series of curcumin-peptide derivatives as PepT1-mediated transport drugs
Zhang, Jiyun,Wen, Hongmei,Shen, Fei,Wang, Xinzhi,Shan, Chenxiao,Chai, Chuan,Liu, Jian,Li, Wei
, (2019/08/26)
Curcumin (CUR) is a natural yellow pigment from turmeric with extensive bioactivities. However its relatively poor solubility limited its absorption and bioavailability. In this study, a novel series of CUR-peptide conjugates were designed and synthesized
Sequential One-Pot Synthesis of Dipeptides through the Transient Formation of CDI-N-Protected α-Aminoesters
de Figueiredo, Renata Marcia,Suppo, Jean-Simon,Midrier, Camille,Campagne, Jean-Marc
supporting information, p. 1963 - 1968 (2017/06/09)
The synthesis of dipeptides through a sequential one-pot procedure from commercially available protected amino acids is described. The transformation relies on the use of in situ generated transiently CDI-protected α-amino esters (CDI, e.g. N,N′-carbonyldiimidazole). In addition of being a highly atom-economical process, the couplings take place under very mild and neutral conditions without adding a base to the reaction medium. This protocol provides a concise and less costly route to dipeptide derivatives (12 examples, up to 87% yield) and is compatible with commonly used N-urethane protecting groups. Moreover, no epimerization was detected even when sensitive Boc-Cys(Bn)?OH was used. (Figure presented.).