- Benzo-five-membered heterocycle HPPD inhibitor or salt thereof, herbicide composition, preparing method and application
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The invention discloses a benzo-five-membered heterocycle HPPD inhibitor or a salt thereof with a formula I or II, a herbicide composition, a preparing method and application. X in the formula I or IIrepresents a nitrogen atom, an oxygen atom or a sulphur atom; R1 represents a hydrogen atom, C1-6 alkyl, C1-6 alkoxy and aromatic groups; R2 and R3 represent halogen, nitryl, trifluoromethyl, cyano group, sulfone methyl, C1-6 alkyl or C1-6 alkoxy; R4 in the formula I represents a hydrogen atom or methyl; R4 in the formula II represents a hydrogen atom, cyclopropyl, trifluoromethyl, C1-6 alkyl orC1-6 alkoxy; R5 in the formula II represents a hydrogen atom, C1-6 alkyl, C1-6 alkoxy or aromatic rings. According to the benzo-five-membered heterocycle HPPD inhibitor or the salt thereof with the formula I or II, the herbicide composition, the preparing method and application, an organic framework completely different from those of marketized HPPD inhibitors is constructed, and the bioassay activity is equivalent to that of mesotrione. When the inhibitor is used as a herbicide, the growth inhibition effect is significant.
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Paragraph 0046-0051
(2019/10/22)
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- Palladium-Catalyzed Intramolecular Arylative Carboxylation of Allenes with CO2 for the Construction of 3-Substituted Indole-2-carboxylic Acids
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Arylative carboxylation of allenes proceeded in an intramolecular manner to afford the corresponding β,γ-unsaturated carboxylic acids in high yields using PdCl2/PAr3 (Ar = C6H4-p-CF3) and ZnEt2 under 1 atm of CO2. The intermediate of the cyclization/carboxylation sequence is thought to be a nucleophilic η1-allylethylpalladium, which reacts with CO2 at the γ-position of palladium. The products obtained could be efficiently converted into 3-substituted indole-2-carboxylate derivatives. One-pot synthesis of strychnocarpine, a β-carboline alkaloid, from the carboxylated product was also demonstrated.
- Higuchi, Yuki,Mita, Tsuyoshi,Sato, Yoshihiro
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supporting information
p. 2710 - 2713
(2017/05/24)
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- Rhodium(III)-catalyzed redox-neutral coupling of N-phenoxyacetamides and alkynes with tunable selectivity
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Give it a tweak: A novel oxidizing directing group was developed for a rhodium(III)-catalyzed C-H functionalization of N-phenoxyacetamides with alkynes. A small change in the reaction conditions leads to either ortho-hydroxyphenyl-substituted enamides or cyclization to deliver benzofurans with high selectivity (see scheme; Cp=C5Me5). Copyright
- Liu, Guixia,Shen, Yangyang,Zhou, Zhi,Lu, Xiyan
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p. 6033 - 6037
(2013/07/19)
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- BENZOFURAN ANILIDE HISTONE DEACETYLASE INHIBITORS
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The present disclosure provides a compound of general Formula (I) having enzyme inhibitory activity, a pharmaceutical composition comprising the compound, and a method useful to treat diseases using the compound.
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Page/Page column 29-30
(2009/07/18)
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- HETEROCYCLIC DERIVATIVES FOR MODULATION OF CALCIUM CHANNELS
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Heterocyclic derivatives act as Ca channel antagonists. The compositions are useful for treating or relieving Ca channel mediated conditions.
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Page/Page column 167
(2008/06/13)
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- NOVEL SAFRAMYCIN ANALOGS AS THERAPEUTIC AGENTS
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The present invention is directed to saframcyin analogs that are useful in the treatment of cancer. Pharmaceutical compositions and processes for preparing these compounds are also disclosed.
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Page/Page column 80-81
(2010/02/15)
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- ACETYLENE DERIVATIVES AS INHIBITORS OF HISTONE DEACETYLASE
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The present invention is directed to certain hydroxamate derivatives that are inhibitors of histone deacetylase and are therefore useful in the treatment of diseases associated with histone deacetylase activity. Pharmaceutical compositions and processes for preparing these compounds are also disclosed.
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Page/Page column 43
(2010/02/11)
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- Identification of MK-944a: A second clinical candidate from the hydroxylaminepentanamide isostere series of HIV protease inhibitors
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Recent results from human clinical trials have established the critical role of HIV protease inhibitors in the treatment of acquired immune-deficiency syndrome (AIDS). However, the emergence of viral resistance, demanding treatment protocols, and adverse side effects have exposed the urgent need for a second generation of HIV protease inhibitors. The continued exploration of our hydroxylaminepentanamide (HAPA) transition-state isostere series of HIV protease inhibitors, which initially resulted in the identification of Crixivan (indinavir sulfate, MK-639, L-735,524), has now yielded MK-944a (L-756,423). This compound is potent, is selective, and competitively inhibits HIV-1 PR with a K(i) value of 0.049 nM. It stops the spread of the HIV(IIIb)-infected MT4 lymphoid cells at 25.0-50.0 nM, even in the presence of α1 acid glycoprotein, human serum albumin, normal human serum, or fetal bovine serum. MK-944a has a longer half-life in several animal models (rats, dogs, and monkeys) than indinavir sulfate and is currently in advanced human clinical trials.
- Dorsey,McDonough,McDaniel,Levin,Newton,Hoffman,Darke,Zugay-Murphy,Emini,Schleif,Olsen,Stahlhut,Rutkowski,Kuo,Lin,Chen,Michelson,Holloway,Huff,Vacca
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p. 3386 - 3399
(2007/10/03)
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- Synthesis and Evaluation of 2-Pyridinone Derivatives as HIV-1-Specific Reverse Transcriptase Inhibitors. 2. Analogues of 3-Aminopyridin-2(1H)-one
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A series of nonnulceoside 3-aminopyridin-2(1H)-one derivatives was synthesized and evaluated for HIV-1 RT inhibitory properties.Several analogs proved to be potent and highly selective antagonists with in vitro IC50 values as low as 19 nM in the enzyme assay using rC*dG as template*primer.Two compounds from this series, 3-amino>-5-ethyl-6-methylpyridin-2(1H)-one (34, L-697,639) and the corresponding 4,7-dichloro analogue (37, L-697,661) inhibited the spread of HIV-1 IIIb infection by 95percent in MT4 cell culture at concentrations of 25-50 nM and were selected for clinical trials as antiviral agents.
- Saari, Walfred S.,Wai, John S.,Fisher, Thorsten E.,Thomas, Craig M.,Hoffman, Jacob M.,et al.
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p. 3792 - 3802
(2007/10/02)
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- BENZOFURAN DERIVATIVES. I. ON THE EFFECTS OF SUBSTITUENTS IN BENZOFURAN SYNTHESES.
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The Roessing's reaction of 4-substituted 2-acylphenoxyacetic acids give a mixture of benzofurans and 2-benzofurancarboxylic acids. The relative yields of benzofurans and 2-benzofurancarboxylic acids depend on the substituents on the benzene ring of the 2-acylphenoxyacetic acids. Electron-withdrawing substituents such as nitro groups favor the formation of 2-benzofurancarboxylic acids. On the other hand, the formation of benzofurans is favored by the steric hindrance of 2-acyl groups in the reaction of 2-acyl-4-nitrophenoxyacetic acids with anhydrous sodium acetate and acetic anhydride.
- Suzuki,Horaguchi,Shimizu,Abe
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p. 2762 - 2767
(2007/10/02)
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