scholarly journals Development of a Practical Synthesis of the 8-FDC Fragment of OPC-167832

Author(s):  
Vijayagopal Gopalsamuthiram ◽  
Dang Ho ◽  
Cheryl Peck ◽  
Vasudevan Natarajan ◽  
Toolika Agrawal ◽  
...  

A concise and practical synthesis has been developed to provide the 8-fluoro-5-hydroxy-3,4-diydrocarbostyril (8-FDC) fragment of OPC-167832 in 41 % yield and in > 99 % purity over 4 steps from 3-amino-4-fluorophenol. The key feature of this process is the development of a telescoped one pot synthesis of the quinolone via a chemoselective amidation and easier product isolation without the need for a column chromatography.

ChemInform ◽  
2008 ◽  
Vol 39 (40) ◽  
Author(s):  
Takao Kikuchi ◽  
Yusuke Nobuta ◽  
Junko Umeda ◽  
Yasunori Yamamoto ◽  
Tatsuo Ishiyama ◽  
...  

Tetrahedron ◽  
2008 ◽  
Vol 64 (22) ◽  
pp. 4967-4971 ◽  
Author(s):  
Takao Kikuchi ◽  
Yusuke Nobuta ◽  
Junko Umeda ◽  
Yasunori Yamamoto ◽  
Tatsuo Ishiyama ◽  
...  

1998 ◽  
Vol 2 (6) ◽  
pp. 344-350 ◽  
Author(s):  
Masahiko Kinugawa ◽  
Satoru Nagamura ◽  
Akihiko Sakaguchi ◽  
Yoshiaki Masuda ◽  
Hiromitsu Saito ◽  
...  

2007 ◽  
Vol 4 (4) ◽  
pp. 606-610 ◽  
Author(s):  
Rajesh Kumar ◽  
Y. C. Joshi

A series of some imidazolines and benzimidazoles were synthesizedfrom various aldehydes and 1,2-diamines in the presence of ceric(IV)ammonium nitrate (CAN). The title compounds were prepared via one stepsynthesis method. The simplicity of the reaction conditions with shorterreaction time and with out use of column chromatography to get the pureproducts in high yields makes this method more attractive for organic chemists.


ChemInform ◽  
2010 ◽  
Vol 30 (13) ◽  
pp. no-no
Author(s):  
Masahiko Kinugawa ◽  
Satoru Nagamura ◽  
Akihiko Sakaguchi ◽  
Yoshiaki Masuda ◽  
Hiromitsu Saito ◽  
...  

2020 ◽  
Vol 18 (11) ◽  
pp. 2175-2181 ◽  
Author(s):  
Naiguo Xing ◽  
Jiangkun Huang ◽  
Peng Wang ◽  
Lan Luo ◽  
Shilong Zheng ◽  
...  

A new copper-catalyzed one-pot reaction resulted in the practical synthesis of imidazolinones from esters.


Author(s):  
Mukund G Kulkarni ◽  
Sanjay W Chavhan ◽  
Mahadev P Shinde ◽  
Dnyaneshwar D Gaikwad ◽  
Ajit S Borhade ◽  
...  

A zeolite-catalyzed, simple, one-pot, solvent-free, cost effective, and environmentally benign process for the synthesis of dihydropyrimidones is described. This reaction is scaleable to multigram scale and the catalyst is recyclable. This methodology has resulted in an efficient synthesis of monastrol, a potent inhibitor of kinesin Eg5.


2020 ◽  
Author(s):  
Lucien Caspers ◽  
Julian Spils ◽  
Mattis Damrath ◽  
Enno Lork ◽  
Boris Nachtsheim

In this article we describe an efficient approach for the synthesis of cyclic diaryliodonium salts. The method is based on benzyl alcohols as starting materials and consists of an Friedel-Crafts-arylation/oxidation sequence. Besides a deep optimization, particluar focusing on the choice and ratios of the utilized Bronsted-acids and oxidants, we explore the substrate scope of this transformation. We also discuss an interesting isomerism of cyclic iodonium salts substituted with aliphatic substituents at the bridge head carbon. <br>


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