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An Efficient and Facile Synthesis of 5‐(Thiophene‐2‐carbonyl)‐6‐(trifluoromethyl)‐tetrahydro‐pyrimidin‐2(1 H )‐one and 6‐(Thiophen‐2‐yl)‐4,5‐dihydropyrimidin‐2(1 H )‐one from Same Substrates Under Different Conditions
Author(s) -
LiangCe Rong,
Zha Yunyun,
Xia Sheng,
Ji Linlin,
Zhang Jing,
Cai Peijun
Publication year - 2016
Publication title -
journal of heterocyclic chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.321
H-Index - 59
eISSN - 1943-5193
pISSN - 0022-152X
DOI - 10.1002/jhet.2299
Subject(s) - chemistry , trifluoromethyl , thiophene , derivative (finance) , catalysis , organic chemistry , medicinal chemistry , solvent , alkyl , financial economics , economics
A series of 5‐(thiophene‐2‐carbonyl)‐6‐(trifluoromethyl)‐tetrahydropyrimidin‐2(1 H )‐one and 6‐(thiophen‐2‐yl)‐4,5‐dihydropyrimidin‐2(1 H )‐one derivatives have been synthesized from the reactions of aromatic aldehydes, 4,4,4‐trifluoro‐1‐(thien‐2‐yl)butane‐1,3‐dione and urea under the different conditions with high yields. In this research, it was found that the p ‐toluenesulfonic acid was an efficient catalyst for obtaining 5‐(thiophene‐2‐carbonyl)‐6‐(trifluoromethyl)‐tetrahydropyrimidin‐2(1 H )‐one derivative. At the same time, solvent‐free and NaOH were the preferred conditions for the synthesis of 6‐(thiophen‐2‐yl)‐4,5‐dihydropyrimidin‐2(1 H )‐one derivative. Moreover, because of short reaction time, excellent yields, simple setup, this research offered an efficient process for preparing these kind compounds.