| 摘要 |
The present invention relates to a novel process for the preparation of compounds of general formula (I);
and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids and bases, which have valuable pharmacological properties, particularly an inhibitory effect on epithelial sodium channels, the use thereof for the treatment of diseases, particularly diseases of the lungs and airways. |
| 主权项 |
1. A process for the preparation of compounds of general formula (III) optionally in the form of a tautomer or acid addition salt thereof,
characterised in that the process comprises reaction step (C), wherein (C) is the reaction of a tertiary alcohol selected from tert-butanol, 2-methyl-2-butanol, 2-methyl-2-pentanol, 2-methyl-2-hexanol, 2,3-dimethyl-2-butanol or 2,4-dimethyl-2-pentanol;
and5-methyl-1,2-oxazolein the presence of an acid of formula XHand a compound of formula (V)
R1—COOH (V)without isolation of a compound of formula (II) to form a compound of formula (III) wherein
XH denotes an acid selected from among HPF6, HBF4, HSbF6, phenylsulphonic acid, p-toluenesulphonic acid, H2SO4, (H2SO4)/2, F3CCOOH, FSO3H, or F3CSO3H;R1 denotes a group of formula (i), wherein
A1 and A2 independently from each other denote N or CH;R1.1 denotes a group selected from among hydrogen, chloro, bromo or methyl,R1.2 denotes a group selected from among hydrogen, amino, C1-3-alkyl-NH—, (C1-3-alkyl)2N— or methyl, or
R1.1 and R1.2 together form an annelated benzo ring; andRt denotes C1-4-alkyl. |
