26815-04-3Relevant articles and documents
Evaluation of 2-(piperidine-1-yl)-ethyl (PIP) as a protecting group for phenols: Stability to ortho-lithiation conditions and boiling concentrated hydrobromic acid, orthogonality with most common protecting group classes, and deprotection via Cope elimination or by mild Lewis acids
Norén, Rolf
, (2021/04/07)
A new protecting group, 2-(piperidine-1-yl)-ethyl (PIP), was evaluated as a protecting group for phenols. The PIP group was stable to ortho-lithiation conditions and refluxing with concentrated hydrobromic acid. Deprotection was accomplished by two routes, oxidation to N-oxides followed by Cope elimination (CE) and subsequent hydrolysis or ozonolysis of the vinyl ether or one-step deprotection by BBr3?Me2S. The PIP group is orthogonal to the O-benzyl, O-acetyl, O-t-butyldiphenylsilyl, O-methyl, O-p-methoxybenzyl, O-allyl, O-tetrahydropyranyl and N-t-butoxy carbonyl groups. The CE step was systematically studied and was found to give higher yields when the reaction was performed in the presence of silylating agents.
TOLL-LIKE RECEPTOR SIGNALING INHIBITORS
-
Paragraph 00307, (2019/07/20)
Di- and triaryl-substituted heteroaromatic compounds have Toll-like receptor inhibitory activity, including at TLR2, TLR4, TLR7, and/or TLR9. Compounds and compositions have applications in the treatment of diseases and conditions mediated by Toll-like receptors and related receptors, such as bacterial sepsis, autoimmune disease, lupus erythematosus, ischemia-reperfusion injury, stroke, metabolic disease, obesity-related metabolic inflammation, gout, and cancer.
Development of chalcone-O-alkylamine derivatives as multifunctional agents against Alzheimer's disease
Bai, Ping,Wang, Keren,Zhang, Pengfei,Shi, Jian,Cheng, Xinfeng,Zhang, Qi,Zheng, Cheng,Cheng, Yao,Yang, Jian,Lu, Xiaoxia,Sang, Zhipei
, (2019/10/02)
A series of novel chalcone-O-alkylamine derivatives were designed, synthesized and evaluated as multifunctional anti-Alzheimer's disease agents. Based on the experimental results, compound 23c exhibited good inhibitory potency on both acetylcholinesterase