494841-92-8Relevant academic research and scientific papers
Potent and orally active ETA selective antagonists with 5,7-diarylcyclopenteno[1,2-b]pyridine-6-carboxylic acid structures
Yoshizumi, Takashi,Takahashi, Hirobumi,Ohtake, Norikazu,Jona, Hideki,Sato, Yoshiyuki,Kishino, Hiroyuki,Sakamoto, Toshihiro,Ozaki, Satoshi,Takahashi, Hiroyuki,Shibata, Yoshihiro,Ishii, Yasuyuki,Saito, Michiyasu,Okada, Megumu,Hayama, Takashi,Nishikibe, Masaru
, p. 2139 - 2150 (2007/10/03)
The synthesis and structure-activity relationships of a series of 5,7-diarylcyclopenteno[1,2-b]pyridine-6-carboxylic acids are described. Our efforts have been focused on modification of the aryl ring at the 5-position and the alkyl substituent at the 2-p
Asymmetric synthesis of a selective endothelin A receptor antagonist
Kato, Yoshiaki,Niiyama, Kenji,Nemoto, Takayuki,Jona, Hideki,Akao, Atsushi,Okada, Shigemitsu,Song, Zhiguo J,Zhao, Matthew,Tsuchiya, Yoshimi,Tomimoto, Koji,Mase, Toshiaki
, p. 3409 - 3415 (2007/10/03)
An asymmetric synthesis of a selective endothelin A receptor antagonist 1b is described. A highly substituted pyridine intermediate 11a was efficiently prepared via a mono-amination of inexpensive 2,6-dichloropyridine followed by a Vilsmeier formylation.
Asymmetric synthesis of a selective endothelin a receptor antagonist
Kato, Yoshiaki,Niiyama, Kenji,Jona, Hideki,Okada, Shigemitsu,Akao, Atsushi,Hiraga, Shouichi,Tsuchiya, Yoshimi,Tomimoto, Koji,Mase, Toshiaki
, p. 1066 - 1072 (2007/10/03)
An asymmetric synthesis of a selective endothelin A receptor antagonist 1b is described. Asymmetric conjugate addition of aryllithium derived from 18 to the chiral oxazoline 17 followed by hydrolysis afforded 15 in 96% ee via purification as (S)-(-)-1-phe
