101892-24-4Relevant academic research and scientific papers
Photoredox Catalyzed Intramolecular Fluoroalkylarylation of Unactivated Alkenes
Zhang, Zuxiao,Martinez, Henry,Dolbier, William R.
, p. 2589 - 2598 (2017/03/14)
The first example of photoredox catalyzed difluoromethylation of unactivated alkenes coupled with C-C bond formation to an aryl ring is reported. The reactions are conducted under mild conditions and afford tetralin derivatives bearing difluoromethyl as well as other fluoroalkyl groups in good to high yields. In addition, the study indicates that 6-exo radical cyclization of an alkyl radical to a phenyl ring is faster than the respective 5-exo radical cyclization. A computational study provides insights to the experimental results.
SAR of 2-benzyl-4-aminopiperidines NK1 antagonists. Part 2. Synthesis of CGP 49823
Veenstra, Siem J.,Hauser, Kathleen,Schilling, Walter,Betschart, Claudia,Ofner, Silvio
, p. 3029 - 3034 (2007/10/03)
CGP 49823 is a potent NK1 antagonist which is centrally active after oral administration. The SAR of the C-2 substituent was investigated with respect to the affinity to the NK1 receptor. A practical synthesis of CGP 49823, suitable for scale-up, was developed. The key-step, a tandem acyliminium ion cyclization/Ritter reaction, gave trans-2-benzyl-4-acetamido-piperidines with high diastereoselectivity.
