131826-72-7Relevant academic research and scientific papers
Synthesis of 2,5-Dioxygenated Pyrazine 4-Oxides: Total Synthesis of a New Inhibitor of Superoxide Anion Generation, OPC-15161
Kita, Yasuyuki,Akai, Shuji,Fujioka, Hiromichi,Tamura, Yasumitsu,Tone, Hitoshi,Taniguchi, Youichi
, p. 875 - 884 (2007/10/02)
The total synthesis of OPC-15161 1, a new inhibitor of superoxide anion generation, is described in full.Three approaches, routes A-C, have been investigated focusing on the pivotal structure 2,5-dioxygenated pyrazine 4-oxide.Among them, route A led to the total synthesis of 1.That is, the key precursor, 5-hydroxypyrazin-2(1H)-one 4-oxide 7 has been prepared from tryptophan methyl ester 2 in three steps, and direct methylation of the 5-hydroxy group of 7 or three-step methylation via the 2-O-Boc derivative 10 afforded 1 in 9.9-10.6percent overall yields.
Indole derivatives
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, (2008/06/13)
The novel indole derivatives and salts thereof represented by the general formula (1) STR1 possess, for example, an inhibitory effect against superoxide (O2-) released from the macrophage cells of guinea pig by stimulation and an anti-albuminuria activity against Masugi nephritis, and are useful in various clinical fields as an agent for preventing and treating diseases and cases associated with the above superoxide radical, for example, autoimmune diseases (e.g. rheumatism), arteriosclerosis, ischemic disease, ischemic encephalopathia, hepatic insufficiency and renal insufficiency, and also as an agent for preventing and treating nephritis.
