Process for preparation of temozolomide

Process for preparation of temozolomide

The invention relates to a method for industrially preparing temozolomide on a large scale, and the key intermediate 5-amino-N1-imidazole-1, 4-dicarboxamide (carbamoyl-AICA) is prepared by adopting N-methyl carbamoyl imidazole (NMCI) type I. In addition, the present invention relates to a process fo...

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Bibliographische Detailangaben
Hauptverfasser: MASSONI MARCO, CECCATO, MARCELO, DE SIO VINCENZO, PACHECO, OGARI DE CASTRO
Format: Patent
Sprache:chi ; eng
Schlagworte:
CHEMISTRY
HETEROCYCLIC COMPOUNDS
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
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Beschreibung
Zusammenfassung:The invention relates to a method for industrially preparing temozolomide on a large scale, and the key intermediate 5-amino-N1-imidazole-1, 4-dicarboxamide (carbamoyl-AICA) is prepared by adopting N-methyl carbamoyl imidazole (NMCI) type I. In addition, the present invention relates to a process for the preparation of NMCI type I. The NMCI type I and temozolomide are purified by crystallization without the use of a chromatographic column or continuous extraction. 本发明涉及以工业大规模制备替莫唑胺的方法，其中采用N-甲基氨基甲酰基咪唑(NMCI)I型来制备关键中间体5-氨基-N1-咪唑-1,4-二甲酰胺(氨基甲酰基-AICA)。此外，本发明涉及制备I型NMCI的方法。NMCI I型与替莫唑胺通过结晶来纯化，而无需使用色谱柱或连续提取。