469-22-7Relevant articles and documents
Nickel-Catalyzed Enantioselective Carbamoyl Iodination: A Surrogate for Carbamoyl Iodides
Abel-Snape, Xavier,Glorius, Frank,Lautens, Mark,Marchese, Austin D.,Mirabi, Bijan,Whyte, Andrew,Wollenburg, Marco
, p. 4780 - 4785 (2020/05/19)
This work reports the enantioselective formal transfer of a carbamoyl iodide across a 1,1-disubstituted styrene using Ni-catalysis. Employing an air-stable Ni(II) precatalyst and a commercially available chiral ligand ((S)-tBuPHOX), enantioenriched 3,3-disubstituted iodooxindoles were obtained in up to 90% yield and up to 97:3 e.r. This methodology was applied to the total synthesis of (-)-esermethole and (-)-phenserine.
Synthesis of physostigmine analogues and evaluation of their anticholinesterase activities
Zhan, Zha-Jun,Bian, Hong-Ling,Wang, Jian-Wei,Shan, Wei-Guang
scheme or table, p. 1532 - 1534 (2010/06/21)
A series of physostigmine analogues were prepared and evaluated for cholinesterase inhibition activities, including acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). Most of them showed potent inhibition activities against AChE, in which compound 17 especially exhibited significantly higher selectivity over BChE than phenserine, a compound currently on clinical trial. Discussion about the relationships between structure and activity of these derivatives was also presented.
An efficient O-dealkylation procedure for the synthesis of (3aS,cis)- 1,2,3,3a,8,8a-hexahydro-1,3a,8-trimethylpyrrolo[2,3-b]indol-5-yl-3,4-dihydro- 2(1H)-isoquinolinecarboxylate
Gao, Zhongli,Lee, Thomas B. K.,Rauckman, Barbara S.
, p. 331 - 333 (2007/10/03)
The title compound is synthesized in high yields and purity from (-)- eserethole (2a) via a lithium bromide catalyzed hydrobromic acid O- dealkylation procedure as the key step.