Categories: Synthesis of N-Heterocycles >
Synthesis of pyrazolines
Recent Literature

A one-pot synthesis of nitrogen-containing heterocycles from alkyl dihalides
and primary amines and hydrazines occurs under microwave irradiation via a
simple and efficient cyclocondensation in an alkaline aqueous medium.
Y. Ju, R. S. Varma, J. Org. Chem., 2006, 71, 135-141.

Arylhydrazines regioselectively react with 3-butynol in the presence of a
catalytic amount of zinc triflate to give aryl-substituted pyrazolines. The
resulting products are easily oxidized in a one-pot procedure to the
corresponding pyrazoles.
K. Alex, A. Tillack, N. Schwarz, M. Beller, Org. Lett., 2008,
10, 2377-2379.

Various 1-acyl-5-hydroxy-4,5-dihydro-1H-pyrazoles have been prepared in
good yields from the corresponding 2-alkyn-1-ones. The resulting
dihydropyrazoles undergo dehydration and iodination in the presence of ICl and
Li2CO3 at room temperature to provide 1-acyl-4-iodo-1H-pyrazoles.
J. P. Waldo, S. Mehta, R. C. Larock, J. Org. Chem., 2008,
73, 6666-6670.

A novel, efficient, and general domino reaction of 2-acylaziridines with the
Huisgen zwitterions furnishes 2-pyrazolines. A possible mechanism for the domino
sequence is proposed.
S.-L. Cui, J. Wang, Y.-G. Wang, Org. Lett., 2008,
10, 13-16.
