A Practical Synthesis of Optically Active Platelet-Activating Factor Antagonist, (+)-6-(2-Chlorophenyl)-3-cyclopropanecarbonyl-8, 11-dimethyl-2, 3, 4, 5-tetrahydro-8H-pyrido[4', 3' : 4, 5]thieno[3, 2-f][1, 2, 4]triazolo[4, 3-a][1, 4]diazepine (E6123), and Its Absolute onfiguration

Shuhei MIYAZAWA; Kazuo OKANO; Naoyuki SHIMOMURA; Tetsuya KAWAHARA; Osamu ASANO; Hiroyuki YOSHIMURA; Takatoshi KAWAI; Shigeru SOUDA; Yutaka YOSHIDA; Tadashi SATO; Yoshimasa MACHIDA; Isao YAMATSU

doi:10.1248/cpb.40.521

Shuhei MIYAZAWA, Kazuo OKANO, Naoyuki SHIMOMURA, Tetsuya KAWAHARA, Osamu ASANO, Hiroyuki YOSHIMURA, Takatoshi KAWAI, Shigeru SOUDA, Yutaka YOSHIDA, Tadashi SATO, Yoshimasa MACHIDA, Isao YAMATSU

Author information

Keywords: platelet activating factor, platelet activating factor antagonist, triazolothienodiazepine, E6123, optical resoltion

JOURNAL FREE ACCESS

1992 Volume 40 Issue 2 Pages 521-523

DOI https://doi.org/10.1248/cpb.40.521

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Abstract

Optically active platelet-activating factor (PAF) receptor antagonist, (+)-6-(2-chlorophenyl)-3-cyclopropanecarbonyl-8, 11-dimethyl-2, 3, 4, 5-tetrahydro-8H-pyrido[4', 3' : 4, 5]thieno[3, 2-f][1, 2, 4]triazolo[4, 5-a][1, 4]diazepine (E6123), was synthesized on large-scale by optical resolution using (+)-dibenzoyl-D-tartaric acid. An X-ray crystallographic analysis clearly indicated that the absolute configuration of the synthesized E6123 was S.

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