2145-87-1Relevant academic research and scientific papers
Continuous Flow Synthesis of Urea-Containing Compound Libraries Based on the Piperidin-4-one Scaffold
Riesco-Domínguez, Alejandra,Blanco-Ania, Daniel,Rutjes, Floris P. J. T.
supporting information, p. 1312 - 1320 (2018/04/02)
The advantages of performing reactions in continuous flow vs. the classic batch processes render flow chemistry a suitable technique for library synthesis. Inspired by our recent work to create fluorine-containing nitrogen heterocycles and by the potentia
Synthesis, Herbicidal Activity, and QSAR of Novel N-Benzothiazolyl- pyrimidine-2,4-diones as Protoporphyrinogen Oxidase Inhibitors
Zuo, Yang,Wu, Qiongyou,Su, Sun-Wen,Niu, Cong-Wei,Xi, Zhen,Yang, Guang-Fu
, p. 552 - 562 (2016/02/05)
Protoporphyrinogen oxidase (PPO, E.C. 1.3.3.4) is known as a key action target for several structurally diverse herbicides. As a continuation of our research work on the development of new PPO-inhibiting herbicides, a series of novel 3-(2′-halo-5′-substituted-benzothiazol-1′-yl)-1-methyl-6-(trifluoromethyl)pyrimidine-2,4-diones 9 were designed and synthesized. The bioassay results indicated that a number of the newly synthesized compounds exhibited higher inhibition activity against tobacco PPO (mtPPO) than the controls, saflufenacil and sulfentrazone. Compound 9F-5 was identified as the most potent inhibitor with a Ki value of 0.0072 ΜM against mtPPO, showing about 4.2-fold and 1.4-fold higher potency than sulfentrazone (Ki = 0.03 ΜM) and saflufenacil (Ki = 0.01 ΜM), respectively. An additional green house assay demonstrated that compound 9F-6 (Ki = 0.012 ΜM) displayed the most promising postemergence herbicidal activity with a broad spectrum even at a concentration as low as 37.5 g of active ingredient (ai)/ha. Maize exhibits relative tolerance against compound 9F-6 at the dosage of 150 g ai/ha, but it is susceptible to saflufenacil even at 75 g ai/ha. Thus, compound 9F-6 exhibits the potential to be a new herbicide for weed control in maize fields.
Pyrimidine diketone compounds containing benzoxazine ring and application thereof
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Paragraph 0098; 0099; 0100, (2016/10/07)
The invention discloses a kind of pyrimidine diketone compounds containing a benzoxazine ring and application thereof. The pyrimidine diketone compounds containing the benzoxazine ring are compounds with the structure shown as a general formula (1) in the specification, and in the formula (1), R1 is selected from hydrogen or an alkyl with the carbon atom number of 1-6, R2 is an ester with the carbon atom number of 2-10, and X is selected from halogen. The pyrimidine diketone compounds containing the benzoxazine ring possess high weeding activity.
Pyrimidinedione compound and application thereof
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Paragraph 0114; 0115; 0116, (2016/10/08)
The present invention discloses a pyrimidinedione compound and an application thereof. The pyrimidinedione compound is a compound of the structure shown in the formula (1), wherein in the formula (1), R is selected from an alkyl group with 1 to 6 carbon atoms, an alkenyl group with 2 to 6 carbon atoms, an alkynyl group with 2 to 6 carbon atoms or an ester group with 2 to 10 carbon atoms; X is selected from halogen; and Y is selected from O or S. The pyrimidindione compound disclosed by the present invention has high herbicidal activity .
Power and structure-variable fluorinating agents. The N-fluoropyridinium salt system
Umemoto, Teruo,Fukami, Shinji,Tomizawa, Ginjiro,Harasawa, Kikuko,Kawada, Kosuke,Tomita, Kyoichi
, p. 8563 - 8575 (2007/10/02)
The usefulness of the N-fluoropyridinium salt system as a source of fluorinating agents was examined by using substituted or unsubstituted N-fluoropyridinium triflates 1-11, N-fluoropyridinium salts possessing other counteranions 1a-d and 3a, and the counteranion-bound salts, N-fluoropyridinium-2-sulfonates 12 and 13. Electrophilic fluorinating power was found to vary remarkably according to the electronic nature of the ring substituents. This power increased as the electron density of positive nitrogen sites decreased, and this was correlated to the pKa values of the corresponding pyridines. By virtue of this variation, it was possible to fluorinate a wide range of nucleophilic substrates differing in reactivity. It is thus possible to fluorinate aromatics, carbanions, active methylene compounds, enol alkyl or silyl ethers, vinyl acetates, ketene silyl acetals, and olefins through the proper use of salts pentachloro 6 through 2,4,6-trimethyl 2, their power decreasing in this order. All the reactions could be explained on the basis of a one-electron-transfer mechanism. N-Fluoropyridinium salts showed high chemoselectivity in fluorination, the extent depending on the reactive moiety. In consideration of these Findings, selective 9α-fluorination of steroids was carried out by reacting 1 with tris(trimethylsilyl ether) 73 of a triketo steroid. Regio- or stereoselectivity in fluorination was determined by a N-fluoropyridinium salt structure. Steric bulkiness of the N-F surroundings hindered the ortho fluorination of phenols and aniline derivatives, while the capacity for hydrogen bonding on the part of the counteranions prompted this process, and the counteranion-bound salts 12 and 13 underwent this fluorination exclusively or almost so. Both bulky N-fluoropyridinium triflates 2 and 7 preferentially attacked the 6-position of the conjugated vinyl ester of a steroid from the unhindered β-direction to give a thermally unstable 6β-fluoro isomer. On the basis of these results, N-fluoropyridinium salts may be concluded to constitute a system that can serve as a source of the most ideal fluorinating agents for conducting desired selective fluorination through fluorinating capacity or structural alteration.
