ERGOLINE DERIVATIVE AND ACID ADDITION SALT THEREOF

摘要

NEW MATERIAL:The 8beta-ergoline derivative of formula I and its acid addition salt. EXAMPLE:5-Methyl-1-(6-methyl-8beta-ergonylmethyl)-3-phenylpyrazole. USE:A drug. A preventive and remedy for hyperprolactinemia, Parkinson disease, etc. It has extremely low side effects such as emesis. It is administered by oral administration at a dose of 0.005-10mg/kg body weight per day. PREPARATION:The compound of formula I can be produced by reacting a compound of formula II (X is eliminable group consisting of an acid residue such as halogen and sulfonyloxy) with 3-methyl-5-phenylpyrazole or its metal salt in a solvent such as dimethyl formamide in the presence of a base such as NaH at 50-140 deg.C for formamide in the presence of a base such as NaH at 50-140 deg.C for 5min-15hr.