AN IMPROVED PROCESS FOR THE PREPARATION OF TEMOZOLOMIDE AND ANALOGS

Disclosed herein is a process for isolating 3-methyl-8-aminocarbonyl-imidazo[5,1-d]-1,2,3,5-terazin-4(3H)-one (temozolomide)comprising diazotizing a compound of formula IIA, wherein R=CH3, in the presence of at least one metal halide, an acid and a source of nitrous acid, wherein the diazotization p...

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Bibliographische Detailangaben
Hauptverfasser: RAO, DHARMARAJ, RAMACHANDRA, KANKAN, RAJENDRA, NARAYANRAO, SRINIVAS, PATHI, L
Format: Patent
Sprache:eng
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Zusammenfassung:Disclosed herein is a process for isolating 3-methyl-8-aminocarbonyl-imidazo[5,1-d]-1,2,3,5-terazin-4(3H)-one (temozolomide)comprising diazotizing a compound of formula IIA, wherein R=CH3, in the presence of at least one metal halide, an acid and a source of nitrous acid, wherein the diazotization proceeds by the addition of the compound of formula IIA and the metal halide to a solution containing the source of nitrous acid and subjecting the acidic solution of temozolomide to a counter-current continuous liquid-liquid extraction using water immiscible solvent.