131185-06-3Relevant articles and documents
Pilot-scale synthesis of a novel non-xanthine adenosine A1 receptor antagonist. 1,3-dipolar cycloaddition of pyridine N-imine to an acetylene
Zanka, Atsuhiko,Hashimoto, Norio,Uematsu, Ryoichi,Okamoto, Takumi
, p. 320 - 324 (2013/09/08)
Adenosine A1 receptor antagonist, FK838, has been synthesized in 44% overall yield by a five-step sequence which is operationally straightforward and readily carried out on a large scale. Investigations into the 1,3-dipolar cycloaddition process that afforded a pyrazolo[1,5-a]pyridine derivative are also described. Process improvements and optimization of each step permitted elimination of column chromatography, resulting in a practical and cost-effective synthesis of FK838. These methods were successfully scaled up in a pharmaceutical pilot plant to give bulk drug used in clinical trials.
NEW USE OF THE ADENOSINE ANTAGONIST
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, (2008/06/13)
The present method for the treatment of pancreatitis, which comprises administering an effective amount of a pyrazolopyridine compound of the following formula: STR1 wherein R 1 is lower alkyl, (substituted) aryl, or a heterocyclic group,R. sup.2 is
Pyrazolopyridine compounds
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, (2008/06/13)
There are disclosed 3 [2(substituted alkyl)-3-oxo-2,3-dihydropyridazin-6-yl]-2-aryl pyrazolo [1,5-a]-pyridines useful for treating maladies requiring an adenosine antagonist, and preparative processes.