Uusi menetelmä 4-metyyli-5-(2-kloori-etyyli)-tiatsolin ja sen analogien valmistamiseksi

The invention relates to 5-(2-chloro-C2-5-alkyl)-4-methyl-1,3-thiazoles of the general formula I, wherein R is a straight-chain 2-chloro-C2-5-alkyl group and a process for their preparation, which is characterized by (A1) reacting a 3-(2-chloro-C2-5-alkyl)-3-thiocyanato-2-propanone of the general fo...

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Hauptverfasser: KISS, PAL, MORASZ, FERENC, SPERBER, FERENC, MOLNAR, ERZSEBET, KOVARI, ARPAD, SZABO, ERZSEBET, HEJA, GERGELY, GYORI, PETER, GARACZY, SANDOR, GOENCZI, CSABA, MIHALOVICS, GYOERGY, SUETO, MIHALY, BONE, ISTVAN, BUTTKAI, ILDIKO, BAN, KAROLY, PALOSI, ENDRE, NEMETH, ATTILA, SZVOBODA, IDA, SZALAY, ERZSEBET, GYURE, KAROLY, LEDNICZKY, LASZLO, KORBONITS, DEZSO
Format: Patent
Sprache:fin ; swe
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Zusammenfassung:The invention relates to 5-(2-chloro-C2-5-alkyl)-4-methyl-1,3-thiazoles of the general formula I, wherein R is a straight-chain 2-chloro-C2-5-alkyl group and a process for their preparation, which is characterized by (A1) reacting a 3-(2-chloro-C2-5-alkyl)-3-thiocyanato-2-propanone of the general formula IV in an organic solvent with gaseous hydrogen chloride to obtain the corresponding 2-chloro-5-(2-chloro-C2-5-alkyl)-4-methyl-1,3-thiazole of the general formula II or (A2) reacting a 3-(2-chloro-C2-5-alkyl)-3-thiocyanato-2-propanone of the above formula IV with an aqueous mineral acid to obtain the corresponding 5-(2-chloro-C2-5-alkyl)-2-hydroxy-4-methyl-1,3-thiazole of the general formula III and reacting the thus obtained compound of the formula III with a halogenating agent to obtain the corresponding 2-chloro-5-(2-chloro-C2-5-alkyl)-4-methyl-1,3-thiazole of the above formula II, and (B) hydrogenating the compound of the general formula II to obtain the 5-(2-chloro-C2-5-alkyl)-4-methyl-1,3-thiazole of the above general formula I. The invention further relates to intermediates for the above process, and pharmaceutical compositions comprising the compounds of formula I.