SYNTHESIS OF TEMOZOLOMIDE AND ANALOGS

PROBLEM TO BE SOLVED: To provide a novel process for the synthesis of Temozolomide of an antitumor compound. SOLUTION: The present invention relates to a novel process for synthesis of an antitumor compound, temozolomide (3-methyl-8-aminocarbonyl-imidazo[5,1-d]-1,2,3,5-tetrazin-4(3H)-one), and to an...

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Bibliographische Detailangaben
Hauptverfasser: HOU DONALD, MAS JANET L, KUO SHENUN
Format: Patent
Sprache:eng
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Zusammenfassung:PROBLEM TO BE SOLVED: To provide a novel process for the synthesis of Temozolomide of an antitumor compound. SOLUTION: The present invention relates to a novel process for synthesis of an antitumor compound, temozolomide (3-methyl-8-aminocarbonyl-imidazo[5,1-d]-1,2,3,5-tetrazin-4(3H)-one), and to an intermediate useful in the novel process. The process for preparation of temozolomide includes a step of diazotizing a temozolomide intermediate having a 1-6C alkyl group, and a protective group easily removable by hydrolysis or hydrogenation. The process further includes a step of hydrolyzing the resulting temozolomide intermediate. COPYRIGHT: (C)2009,JPO&INPIT