An improved synthesis of 5-methylpyrazine-2-carboxylic acid

I Iovel, Y Goldberg, M Shymanska

Index: Iovel, I.; Goldberg, Yu.; Shymanska, M. Organic Preparations and Procedures International, 1991 , vol. 23, # 2 p. 188 - 190

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Citation Number: 3

Abstract

5-Methylpyrazine-2carboxylic acid@) is known to be an intermedk~ te'.~ in the synthesis of Glypizide (Minidiab). This drug is structurally related to the latest generation of sulfonylurea derivatives and is used in the treatment of insulin-independent diabetes3 The known route to 4 involves the oxidation of 2, 5-~ hnethylpyrazine c1) with 402 to mono-N-oxide 5, which with Ac, O, gave 2-acetoxymethyl-5-methylpyrazine (a. Hydrolysis of 6 with aqueous alkali ...