PALLADIUM CATALYZED RING CLOSURE OF TRIAZOLYL TRYPTAMINE

摘要

A new process is described for the synthesis of the triazolyl tryptamine ( alpha ) and related compounds. The process involves a palladium-catalyzed ring closure between a substituted ortho-iodoaniline and a protected 1-alkynol. The process is carried out at high temperature, e.g. 100 DEG C, in a dry inert solvent, e.g., DMF and in the presence of a proton acceptor, e.g., Na2CO3 or a trialkylamine. The triazolyl tryptamine, as well as acid addition salts thereof, is a 5 HT1D receptor agonist having anti-migraine properties.