| 摘要 |
<p>PURPOSE: To obtain the subject novel compound that shows excellent activity to improve the enterokinesis with high safety and is useful for the prevention and treatment of a variety of enterokinesis disorder. CONSTITUTION: This compound is a thiazole derivative of formula I (R<1> is oxypyrrolidyl, hydroxymethylpyrrolidyl or a nitrogen-containing unsaturated heterocyclic ring) or its salt, typically N-methyl -N'-2-[2 -[1-[4-(2 -hydroxyethyl) piperazinyl] methyl]-4 -thiazoyl] methylthio]ethyl 2-nitro -1,1 -ethendiamine. The compound of formula I is prepared, for example, by condensation reaction between a compound of formula II (W is a halogen or an eliminating group; Z is H or a protecting group) and a thiol of formula III, deprotecting the protecting group for amino group as formyl group from the intermediate of formula IV in an organic solvent in the presence of an acid followed by reaction of the deprotection product with 1-methylamino -1-methylthio -2-nitroethylene.</p> |
