Preparation of 5,7-dihydroxy-1,2,4-triazolo[1,5-a]pyrimidine-2-s

Organic compounds -- part of the class 532-570 series – Organic compounds – Pteroyl per se or having -c- – wherein x is chalcogen – bonded...

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C07D40314

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active

050066560

ABSTRACT:
5,7-Dihydroxy-N-(aryl)-1,2,4-triazolo[1,5-a]pyrimidine-2-sulfonamides are prepared by the cyclization of N-(3-(((aryl)amino)sulfonyl)-1H-1,2,4-triazol-5-yl)amines with malonyl halides under acidic conditions. With the addition of a phosphorus oxyhalide, malonic acid can be used in place of the malonyl halides and the 5,7-dihydroxy-1,2,4-triazolo[1,5-a]pyrimidine can be directly converted to the corresponding 5,7-dihalo derivative.

REFERENCES:
patent: 4734123 (1988-03-01), Monte
patent: 4818273 (1989-04-01), Kleschick et al.
patent: 4822404 (1989-04-01), Kleschick
patent: 4904301 (1990-02-01), Pearson et al.

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