199446-36-1Relevant academic research and scientific papers
A trinexapac-and intermediate preparation method
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Paragraph 0056; 0057; 0067; 0068, (2017/08/25)
The invention discloses a preparation method of trinexapac-ethyl and an intermediate thereof. The method comprises the following steps: under the action of an alkali, reacting acetoacetic ester (I) with diethyl maleate to obtain an intermediate (II), cont
Acylcyclohexanedione derivatives as potential in vivo sequential inhibitors of 4-hydroxyphenylpyruvate dioxygenase and GA20 3β-hydroxylase
Huang, Jian-Lin,Liu, Hun-Ge,Yang, Ding-Yah
, p. 927 - 930 (2007/10/03)
Acylcyclohexanedione derivatives have been designed, synthesized, and evaluated for in vitro inhibition activity against the enzyme 4-hydroxyphenylpyruvate dioxygenase (4-HPPD). The biological data demonstrated that 7 is a potent inhibitor of 4-HPPD with
SAR studies of 3-cyclopropanecarbonyloxy-2-cyclohexen-1-one as inhibitors of 4-hydroxyphenylpyruvate dioxygenase
Lin, Yung-Lung,Wu, Chung-Shieh,Lin, Shean-Woei,Huang, Jian-Lin,Sun, Yang-Sheng,Yang, Ding-Yah
, p. 685 - 690 (2007/10/03)
Various 3-cyclopropanecarbonyloxy-2-cyclohexen-1-one 1 derivatives have been synthesized and tested as inhibitors of 4-hydroxyphenylpyruvate dioxygenase (4-HPPD) from pig liver. The inhibition results indicated that well-positioned dicarbonyl groups as well as the cyclopropyl group of 1 were essential for potent inhibition. Substitution at the 2-position of the ring system has a significant effect on inhibitor potency, while the 5-position can undergo substantial variations and retain inhibitor potency. In the compounds examined, 2-chloro substituted 12 is the best inhibitor of all with IC50 of 15 nM, the rest of the synthesized analogues were less potent inhibitors than the parent compound.
