摘要 |
<p>The invention relates to 5-(2-chloro-C2-5-alkyl)-4-methyl-1,3-thiazoles of the general formula I, <CHEM> 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 <CHEM> 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 <CHEM> 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 <CHEM> 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.</p> |
申请人 |
ASTRA AKTIEBOLAG |
发明人 |
PALOSI, ENDRE;KORBONITZ, DEZSOE;MOLNER, ERZSEBET;SZVOBODA, IDA;HEJA, GERGELY;KISS, PAL;GOENCZI, CSABA;MORASZ, FERENC;LEDNICZKY, LASZL;SZABO, ERZSEBET;GYOERI, PETER;SZALAY, ERZSEBET;SPERBER, FERENC;MIHALOVICS, GYOERGY;NEMETH, ATTILA;SUETOE, MIHALY;GYUERE, KAROLY;BONE, ISTVAN;BAN, KAROLY;BUTTKAI, ILDIK;KOEVARI, ARPAD;GARACZY, SANDOR |