Anticoccidials. VI. An Improved Synthesis of 1,6-Dihydro-6-oxo-2-pyrazinecarboxylic Acid 4-Oxide and Some Related Derivatives and Determination of Anticoccidial Activity

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概要

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• 1,6-Dihydro-6-oxo-2-pyrazinecarboxylic acid 4-oxide (1) has been synthesized by two different methods. The first is a hydrolysis of methyl 6-chloro-2-pyrazinecarboxylate 4-oxide, which was in turn obtained from methyl 6-chloro-2-pyrazinecarboxylate by reaction with m-chloroperbenzoic acid. The second is an oxidation of 6-hydroxymethyl-2 (1H)-pyrazinone 4-oxide with nickel peroxide. Compound 1 was converted to amine salts, esters and amides. 6-Methoxy, 6-mercapto and 1-alkyl derivatives were also prepared. The compounds prepared were tested for anticoccidial activity in chickens against Eimeria tenella and marked activity was seen with compound 1 and amine salts of 1. The activity of 1 was counteracted by the simultaneous administration of an equal weight of orotic acid or adenine.

• 社団法人日本薬学会の論文
• 1981-01-25

著者

• 瀬尾 卓司

  Animal Health Products Division Takeda Chemical Industries Ltd.

• 松野 年美

  Animal Health Products Division Takeda Chemical Industries Ltd.

• 今井 欣一

  Animal Health Products Division Takeda Chemical Industries Ltd.

• 真野 光彦

  Animal Health Products Division, Takeda Chemical Industries, Ltd.

関連論文

• Studies on Nucleic Acid Antagonists. I. Syntheses of 5-Phenylazopyrimidines.
• Synthesis and Coronary Vasodilating Activity of 2-Substituted Adenosines
• Synthesis of Compounds related to Inosine 5'-Phosphate and Their Flavor Enhancing Activity. IV. 2-Substituted Inosine 5'-Phosphates
• Synthesis of 6-Methylaminopurine by Thermal Cyclization of 4,6-Bis (methylamino) -5-phenylazopyrimidine
• Anticoccidials. VI. An Improved Synthesis of 1,6-Dihydro-6-oxo-2-pyrazinecarboxylic Acid 4-Oxide and Some Related Derivatives and Determination of Anticoccidial Activity
• Anticoccidials. VII. Synthesis of 4,5-Dihydro-5-oxo-2-pyrazinecarboxylic Acid 1-Oxides
• Anticoccidials. V. Synthesis and Anticoccidial Activity of 2(1H)-Pyrazinone 4-Oxide Derivatives
• Anticoccidials. IV. A Convenient Synthesis of 2(1H)-Pyrazinone 4-Oxide Derivatives
• Anticoccidials. II. Autoxidation and Structural Determination of 1-Benzylamino-3-substituted Guanidines
• Anticoccidials. I. Syntheses and Anticoccidial Activity of 2-Amino-5-aryl-1,3,4-oxadiazoles, 5-Alkoxy-3-aryl-1H-1,2,4-triazoles, and 3-Aryl-⊿^2-1,2,4-triazolin-5-ones
• Structure-Activity Relationship in the Taste Effect of Ribonucleotide Derivatives
• Studies on the Synthesis of Pyrimidine Deoxynucleosides. I. Synthesis of 2', 3'-Dideoxyuridine and 1-(3-Ethylthio-3-deoxy-β-D-xylofuranosyl) uracil
• Synthesis of Purine Nucleosides Using Iodine as Catalyst
• Synthesis of the Glucose Analogs of Inosine-5' Phosphate.
• Synthesis of 5-Substituted Pyrimidine Nucleosides
• Studies on Nucleic Acid Antagonists. VII. Synthesis and Characterization of 1,4,6-Triazaindenes (5H-Pyrrolo[3,2-d]pyrimidines)
• Studies on Nucleic Acid Antagonists. VI. Synthesis of 1,4,6-Triazain-denes(5H-Pyrrolo[3,2-d]pyrimidines)
• Synthesis of Uridine Diphosphate-Glucuronic Acid.
• Synthesis of Uridine Diphosphate-Glucuronic Acid
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