posted on 2005-06-10, 00:00authored byGan B. Bajracharya, Zhibao Huo, Yoshinori Yamamoto
The intramolecular hydroamination of alkynes tethered with
amino group 1 in the presence of catalytic amounts of Pd(PPh3)4 and PPh3 in benzene at 100 °C proceeded smoothly
without the use of any additional acid source to afford five-
and six-membered nitrogen heterocycles 2 in good to excellent yields. A compulsory addition of carboxylic acid as a
cocatalyst was not needed, and the reaction could be carried
out under essentially neutral conditions.