Synthesis of [2‐14C]dezaguanine mesylate (6‐amino‐1,5‐dihydro‐4H‐imidazo[4,5‐c]pyridin‐4‐one‐6‐14C methanesulfonate), a new antitumor agent
作者:
Jon D. Hartman,
Vitauts Alks,
C. C. Huang,
P. Dan Cook,
期刊:
Journal of Labelled Compounds and Radiopharmaceuticals
(WILEY Available online 1986)
卷期:
Volume 23,
issue 1
页码: 35-44
ISSN:0362-4803
年代: 1986
DOI:10.1002/jlcr.2580230105
出版商: John Wiley&Sons, Ltd.
关键词: 3‐Deazaguanine mesylate;dezaguanine mesylate;[6‐14C]6‐Amino‐1,5‐dihydroimidazo[4,5‐c]pyridin‐4‐one methanesulfonate;14C;antitumor;methyl 5‐(chloromethyl)‐1H‐imidazole‐4‐carboxylate;hydrochloride
数据来源: WILEY
摘要:
AbstractDezaguanine mesylate (CI‐908 mesylate, 3‐deazaguanine mesylate, 6‐amino‐1,5‐dihydro‐4H‐imidazo[4,5‐c]pyridin‐4‐one methanesulfonate,7), a new antitumor agent, was labeled in‐the 2‐position by use of a new synthesis to 3‐deazaguanine. Thus, methyl 4‐(hydroxymethyl)‐1‐(triphenylmethyl‐1H‐imidazole‐5‐carboxylate (10) was converted with thionyl chloride to the corresponding chloromethyl‐derivative11, which was treated with [14C]‐potassium cyanide to afford the labeled penultimate intermediate, methyl 5‐(cyanomethyl)‐1H‐imidazole‐4‐carboxylate (12). Ring closure of12with methanolic ammonia and subsequent salt f
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