Author(s):
Zhi-Wei Ma*
,
Xiao-Feng Liu,
Xiao-Pei Chen,
Chuan-Chuan Wang,
Jing-Chao Tao and
Quan-Jian Lv*
Page: [908 - 912] Pages: 5
* (Excluding Mailing and Handling)
A new tertiary amine-thiourea organocatalyst has successfully been developed and applied into the asymmetric Michael addition of pyrazolin-5-one to nitroalkenes. The catalyst system performed well with a low catalyst loading of 5 mol% under mild reaction conditions. A series of synthetically and pharmaceutically useful chiral pyrazolone derivatives was obtained in high yields (up to 95%) with good enantioselectivities (up to 88 % ee).
Keywords: Pyrazolone derivatives, michael addition, organocatalysis, tertiary amine-thiourea, pyrazolin-5-ones, nitroalkenes.
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