16307-08-7Relevant academic research and scientific papers
I2/TBHP mediated diastereoselective synthesis of spiroaziridines
Ashitha, Kizhakkan Thiruthi,Vinaya, Puthiya Purayil,Krishna, Ajay,Vincent, Deepthy Cheeran,Jalaja, Renjitha,Varughese, Sunil,Somappa, Sasidhar Balappa
supporting information, p. 1588 - 1593 (2020/03/06)
Eventhough spiroheterocycles are considered as emerging drug candidates, synthesis of spiroaziridines has not been well explored so far. Herein, we disclose an efficient I2/TBHP mediated diastereoselective synthesis of N-alkyl spiroaziridines from primary amines and easily accessible α,β-unsaturated ketones. The reaction is also compatible for the synthesis of 2-aroylaziridines.
Catalytic enantioselective cascade Michael/cyclization reaction of 3-isothiocyanato oxindoles with exocyclic α,β-unsaturated ketones: En route to 3,2′-pyrrolidinyl bispirooxindoles
Kayal, Satavisha,Mukherjee, Santanu
supporting information, p. 10175 - 10179 (2016/11/17)
Cascade Michael/cyclization reactions between 3-isothiocyanato oxindoles and exocyclic α,β-unsaturated ketones are shown to proceed efficiently in the presence of a quinine-derived tertiary amino-squaramide catalyst and furnish 3,2′-pyrrolidinyl bispirooxindoles containing two spiro-quaternary and three contiguous stereocenters as a single diastereomer with excellent enantioselectivities (up to 99:1 er).
Design and characterization of optimized adenosine A2A/A 1 receptor antagonists for the treatment of Parkinson's disease
Shook, Brian C.,Rassnick, Stefanie,Wallace, Nathaniel,Crooke, Jeffrey,Ault, Mark,Chakravarty, Devraj,Barbay, J. Kent,Wang, Aihua,Powell, Mark T.,Leonard, Kristi,Alford, Vernon,Scannevin, Robert H.,Carroll, Karen,Lampron, Lisa,Westover, Lori,Lim, Heng-Keang,Russell, Ronald,Branum, Shawn,Wells, Kenneth M.,Damon, Sandra,Youells, Scott,Li, Xun,Beauchamp, Derek A.,Rhodes, Kenneth,Jackson, Paul F.
experimental part, p. 1402 - 1417 (2012/04/04)
The design and characterization of two, dual adenosine A 2A/A1 receptor antagonists in several animal models of Parkinson's disease is described. Compound 1 was previously reported as a potential treatment for Parkinson's disease. Fu
Optimization of arylindenopyrimidines as potent adenosine A2A/A1 antagonists
Shook, Brian C.,Rassnick, Stefanie,Chakravarty, Devraj,Wallace, Nathaniel,Ault, Mark,Crooke, Jeffrey,Barbay, J. Kent,Wang, Aihua,Leonard, Kristi,Powell, Mark T.,Alford, Vernon,Hall, Daniel,Rupert, Kenneth C.,Heintzelman, Geoffrey R.,Hansen, Kristen,Bullington, James L.,Scannevin, Robert H.,Carroll, Karen,Lampron, Lisa,Westover, Lori,Russell, Ronald,Branum, Shawn,Wells, Kenneth,Damon, Sandra,Youells, Scott,Beauchamp, Derek,Li, Xun,Rhodes, Kenneth,Jackson, Paul F.
scheme or table, p. 2868 - 2871 (2010/07/06)
Two reactive metabolites were identified in vivo for the dual A2A/A1 receptor antagonist 1. Two strategies were implemented to successfully mitigate the metabolic liabilities associated with 1. Optimization of the arylindenopyrimidines led to a number of amide, ether, and amino analogs having comparable in vitro and in vivo activity.
ARYLINDENOPYRIMIDINES AND THEIR USE AS ADENOSINE A2a
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Page/Page column 3; 4, (2009/05/29)
This invention relates to novel arylindenopyrimidines A, B, and C, and their therapeutic and prophylactic uses. Disorders treated and/or prevented using these compounds include Parkinson's Disease.
