| 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 ~C, in a d ry 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 additio n salts thereof, is a 5 HT1D receptor agonist having anti-migraine properties.
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