105754-24-3Relevant articles and documents
Cu(II)-catalyzed C-N coupling of (hetero)aryl halides and N-Nucleophiles promoted by α-benzoin oxime
Yuan, Chunling,Zhang, Lei,Zhao, Yingdai
, (2019/11/28)
We first reported the new application of a translate metal chelating ligand α-benzoin oxime for improving Cu-catalyzed C-N coupling reactions. The system could catalyse coupling reactions of (hetero)aryl halides with a wide of nucleophiles (e.g., azoles, piperidine, pyrrolidine and amino acids) in moderate to excellent yields. The protocol allows rapid access to the most common scaαolds found in FDA-approved pharmaceuticals.
Room temperature N-arylation of amino acids and peptides using copper(i) and β-diketone
Sharma, Krishna K.,Sharma, Swagat,Kudwal, Anurag,Jain, Rahul
supporting information, p. 4637 - 4641 (2015/04/27)
A mild and efficient method for the N-arylation of zwitterionic amino acids, amino acid esters and peptides is described. The procedure provides the first room temperature synthesis of N-arylated amino acids and peptides using CuI as a catalyst, diketone as a ligand, and aryl iodides as coupling partners. The method is equally applicable for using relatively inexpensive aryl bromides as coupling partners at 80 °C. Using this procedure, electronically and sterically diverse aryl halides, containing reactive functional groups were efficiently coupled in good to excellent yields.
Bombesin receptor antagonists
-
, (2008/06/13)
Bombesin receptor antagonists are provided which are compounds of formula (I) or pharmaceutically acceptable salts thereof: wherein j, k, l, m, n, q, r, Ar, Ar1, R1, R2, R3, R4, R5, R6 and X are as defined in the description. The compounds of the invention have an affinity for the BB1 receptor and some of them also have affinity for the BB2 receptor. Accordingly they may be useful for the diagnosis, prevention, or treatment of male and female sexual dysfunction. They can also be used in the diagnosis, prevention or treatment of anxiety and panic disorders, social phobia, depression, psychoses, sleeping disorders, memory impairment, pulmonary hypertension, lung repair and lung development disorders, cancer including prostate cancer and pancreatic cancer, hepatic porphyria, gastrointestinal secretory disturbances, gastrointestinal disorders including colitis, Crohn's disease and inflammatory bowel disease, emesis, anorexia, pain, seasonal affective disorders, feeding disorders or pruritus.