34604-60-9Relevant academic research and scientific papers
Redesign of the Synthesis and Manufacture of an Azetidine-Bearing Pyrazine
Hose, David R. J.,Hopes, Phillip,Steven, Alan,Herber, Christian
, p. 241 - 246 (2018)
Commercial route definition for a glucokinase activator called for a re-evaluation of the synthesis and processes used to access multikilogram quantities of a pyrazine building block. The processes developed allowed a literature route to sodium 6-oxo-1H-pyrazine-3-carboxylate to be leveraged. One of these processes consisted of a highly selective decarboxylation that allowed the target building block to be accessed with complete regioselectivity in standard batch processing equipment. The presence of an azetidine ring in the target required the mitigation of impurity liabilities arising from the use of the hydrochloride salt of azetidine as an input material.
AMIDE DERIVATIVES AND DRUGS
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Page 15, (2010/02/08)
The present invention provides an amide derivative represented by the following formula [1]: wherein n represents 0 or 1; X represents CR4 or N; Y represents CR6 or N; Z represents CR7 or N; R1 and R2 may be the same or different and each represents hydrogen, optionally substituted alkyl, acyl, optionally substituted aryl, or an optionally substituted aromatic heterocyclic group; R4, R5, R6 and R7 may be the same or different and each represents hydrogen, halogen, hydroxy, amino, alkyl, haloalkyl, alkoxy, monoalkylamino, dialkylamino, arylalkyl, cyano, or nitro; and R3 represents optionally substituted alkylamino, optionally substituted arylamino, or optionally substituted cyclic amino, or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising them as an active ingredient. The compound of the present invention is useful as a TGF-β inhibitor.
Studies on Pyrazines. 7 (1). The Synthesis of 5-Chloropyrazinecarboxylic Acid
Sato, Nobuhiro,Arai, Shinji
, p. 407 - 408 (2007/10/02)
The titled carboxylic acid (1) was prepared by condensation of 2-furylglyoxal with aminoacetamide followed by chlorination of the resulting 2-hydroxy-5-(2'-furyl)pyrazine (2) and permanganate oxidation.The acid was further converted into methyl ester and 5-hydroxypyrazinecarboxylic acid.
