PURPOSE: To provide a new compound having a remarkably strong vasodepressor activity, reduced in toxicity, excellent in safety and useful as a therapeutic agent for hypertension, etc.
CONSTITUTION: A compound is represented by formula I (R is Cl or Br) and its salt, e.g. (5R,8S,10R)-2-chloro-6-methyl-8-(1,2,4-triazol-1-ylmethyl)ergoline. This compound is obtained by reacting an ergoline derivative [e.g. (5R,8S,10R)-2- chloro-6-methylergolin-8-ylmethyl 4-toluene-sulfonate] of formula II (X is Cl, methanesulfonyloxy, etc.) with 1,2,4-triazole generally in an inert solvent such as THF. This reaction is generally carried out recommendably at room temperatures to 140°C for 5 to 24hr. In addition, the compound of formula II can be synthesized, e.g. by reacting (5R,8S,10R)-2-chloro-6-methylergoline-8- methanol with p-toluenesulfonic acid chloride in the presence of pyridine.
ADACHI YUUKO
TAKAMORI MASAYUKI
MIZUKOSHI SEISHI
NAGASAKA MITSUAKI
ICHIHARA KENJI
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