565453-43-2Relevant academic research and scientific papers
Photoredox-catalyzed deoxyfluorination of activated alcohols with Selectfluor
González-Esguevillas, María,Miró, Javier,Jeffrey, Jenna L.,MacMillan, David W.C.
supporting information, p. 4222 - 4227 (2019/06/13)
Herein we disclose a deoxyfluorination of alcohols with an electrophilic fluorine source via visible-light photoredox catalysis. This radical-mediated C–F coupling is capable of fluorinating secondary and tertiary alcohols efficiently, complementing previously reported nucleophilic deoxyfluorination protocols.
Naphthoquinone derivative containing adamantyl and preparation method and application of derivative
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Paragraph 0159-0161, (2017/01/05)
The invention provides a naphthoquinone derivative containing adamantyl and a preparation method and application of the derivative, and particularly provides a naphthoquinone derivative which is as shown in a following formula (I) and contains adamantyl, wherein definitions of all groups are described in the description. The compound has Sortase A enzyme inhibitory activity and cytotoxic activity and can be used for treating diseases related to Sortase A enzyme and various malignant tumors. Please see the formula (I) in the description.
1-[[(3-Hydroxy-1-adamantyl)amino]acetyl]-2-cyano-(S)-pyrrolidine: A potent, selective, and orally bioavailable dipeptidyl peptidase IV inhibitor with antihyperglycemic properties
Villhauer, Edwin B.,Brinkman, John A.,Naderi, Goli B.,Burkey, Bryan F.,Dunning, Beth E.,Prasad, Kapa,Mangold, Bonnie L.,Russell, Mary E.,Hughes, Thomas E.
, p. 2774 - 2789 (2007/10/03)
Dipeptidyl peptidase IV (DPP-IV) inhibition has the potential to become a valuable therapy for type 2 diabetes. The synthesis and structure - activity relationship of a new DPP-IV inhibitor class, N-substituted-glycyl-2-cyanopyrrolidines, are described as well as the path that led from clinical development compound 1-[2-[5-cyanopyridin-2-yl)amino]ethylamino]acetyl-2-cyano-(S)pyrrolidine (NVP-DPP728, 8c) to its follow-up, 1-[[(3-hydroxy-1-adamantyl)amino]acetyl]-2-cyano-(S)pyrrolidine (NVP-LAF237, 12j). The pharmacological profile of 12j in obese Zucker fa/fa rats along with pharmacokinetic profile comparison of 8c and 12j in normal cynomolgus monkeys is discussed. The results suggest that 12j is a potent, stable, selective DPP-IV inhibitor possessing excellent oral bioavailability and potent antihyperglycemic activity with potential for once-a-day administration.
