- A continuous flow synthesis of [1.1.1]propellane and bicyclo[1.1.1]pentane derivatives
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A continuous flow process to generate [1.1.1]propellane on demand is presented rendering solutions of [1.1.1]propellane that can directly be derivatised into various bicyclo[1.1.1]pentane (BCP) species. This was realised in throughputs up to 8.5 mmol h-1providing an attractive and straightforward access to gram quantities of selected BCP building blocks. Lastly, a continuous photochemical transformation of [1.1.1]propellane into valuable BCPs bearing mixed ester/acyl chloride moieties was developed.
- Donnelly, Kian,Baumann, Marcus
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supporting information
p. 2871 - 2874
(2021/03/23)
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- Synthesis and application of oxalic acid monoester derivatives
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The invention relates to synthesis and application of oxalic acid monoester-containing compounds as shown in a general formula (I) which is described in the specification. The compounds represent a broad-spectrum efficient insecticidal and bactericidal agent structure type. The oxalic acid monoester-containing compounds can well control aphids, plutella xylostella and spodoptera exigua when used as novel insecticidal bactericides; the compounds can also be used for preventing and treating cucumber brown blotch, cucumber bacterial angular leaf spot, cucumber fusarium wilt, cucumber downy mildew, cucumber powdery mildew, tomato bacterial leaf spot and rice sheath blight. R in the general formula (I) is as defined in the specification.
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Paragraph 0015-0018
(2020/12/08)
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- METHOD OF MAKING PRODRUG FOR SUSTAINED AND CONTROLLED RELEASE
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A novel ROS-responsive prodrug is provided. The prodrug utilizes a unique modified oxalate linker conjugated to 4-aminophenol, which can enhance the reaction kinetics for intracellular ROS within tumor tissues while keeping the modified oxalate backbone stable with amide bond under very low ROS level.
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Paragraph 86
(2020/10/20)
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- A General Strategy Toward Highly Fluorogenic Bioprobes Emitting across the Visible Spectrum
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A general approach toward highly fluorogenic probes across the visible spectrum for various analytes offers significant potential for engineering a wide range of bioprobes with diverse sensing and imaging functions. Here we show a facile and general strategy that involves introducing a new fluorogenic mechanism in boron dipyrromethene (BODIPY) dyes, based on the principle of stimuli-triggered dramatic reduction in the electron-withdrawing capabilities of the meso-substituents of BODIPYs. The fluorogenic mechanism has been demonstrated to be applicable in various BODIPYs with emission maxima ranging from green to far red (509, 585, and 660 nm), and the synthetic strategy allows access to a panel of highly fluorogenic bioprobes for various biomolecules and enzymes (H2O2, H2S, and protease) via introducing specific triggering motifs. The potency of the general design strategy is exemplified by its application to develop a mitochondria-targeting far-red probe capable of imaging of endogenous H2O2 in living cells.
- Chen, Haoliang,He, Xiujing,Su, Meihui,Zhai, Wenhao,Zhang, Hao,Li, Changhua
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supporting information
p. 10157 - 10163
(2017/08/02)
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- BODIPY-based high-sensitivity fluorescent probe and synthesis method and application thereof
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The invention relates to a BODIPY-based high-sensitivity fluorescent probe and a synthesis method and application thereof. A structural general formula of the probe is shown as (I), wherein Trigger is stimulant triggering groups, R1 and R2 are groups for regulating and controlling fluorescent transmission wavelength of the probe and introducing organelle targeting, and R1 and R2 are defined in the description. By the probe, detection of different substrates can be realized without changing mother nucleus structure of the probe by only changing different Trigger groups. In addition, according to different needs on wavelength and targeting, the mother nucleus structure of the probe can be quickly modified. By changing R1 and R2, maximum fluorescent emission wavelength of the probe can be changed, and the probe can target mitochondrion to realize detection of active substances in the mitochondrion. The probe has good biocompatibility, thereby being applicable to detecting biological systems. Application value of the fluorescent probe in the aspect of detecting bioactive molecules and protease over-expressed in inflammatory or tumor tissue has potential social benefit and economic benefit.
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Paragraph 0034-0038
(2018/03/24)
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- Ionic liquids based on oxalic acid mono amides
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The present invention relates to monosubstituted oxalic acid amides of the general formula (I) ????????[A]+ [O-C(O)-C(O)-X]-?????(I) wherein the meaning is for [A]+ a cation made from an organic moiety A having a formally positively charged heteroatom selected from the group consisting of nitrogen, phosphorus and sulfur and X is the group -NRaRb, wherein Ra and Rb are the same or different and are independently from each other hydrogen or a C1 to C30 organic residue with the proviso that at least one of Ra and Rb is a C1 to C30 organic residue.
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Paragraph 0127; 0128
(2015/11/24)
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- Design, synthesis and insecticidal activities of novel N-oxalyl derivatives of neonicotinoid compound
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Ten novel neonicotinoid derivatives containing N-oxalyl groups were designed and synthesized, and their structures were characterized by 1H NMR, MS, IR, elemental analysis and single crystal X-ray diffraction analysis. The insecticidal activities of the new compounds were evaluated. The results of bioassays indicated that some of these title compounds exhibited excellent insecticidal activities.
- Zhao, Yu,Wang, Gang,Li, Yongqiang,Wang, Suhua,Li, Zhengming
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experimental part
p. 475 - 479
(2010/10/20)
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- Synthesis, crystal structure, and insecticidal activity of novel N-alkyloxyoxalyl derivatives of 2-arylpyrrole
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Two series of novel N-alkyloxyoxalyl derivatives of 2-arylpyrrole were synthesized, and their structures were characterized by 1H NMR spectroscopy, elemental analysis, and single-crystal X-ray diffraction analysis. The insecticidal activities of the new compounds were evaluated. The results of bioassays indicated that some of these title compounds exhibited excellent insecticidal activities, and their insecticidal activities against oriental armyworm, mosquito, and spider mite are comparable to those of the commercialized Chlorfenapyr.
- Zhao, Yu,Mao, Chunhui,Li, Yongqiang,Zhang, Pengxiang,Huang, Zhiqiang,Bi, Fuchun,Huang, Runqiu,Wang, Qingmin
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experimental part
p. 7326 - 7332
(2010/06/11)
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- Asymmetric 1,3-dipolar cycloadditions of 2-diazocyclohexane-1,3-diones and alkyl diazopyruvates
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The 1,3-dipolar cycloaddition reactions of 2-diazocyclohexane-1,3-dione (7a; Table 1) and of alkyl diazopyruvates (11a-e; Table 3) to 2,3-dihydrofuran and other enol ethers have been investigated in the presence of chiral transition metal catalysts. With RhII catalysts, the cycloadditions were not enantioselective, but those catalyzed by [RuIICl 2(1a)] and [RuIICl2(1b)] proceeded with enantioselectivities of up to 58% and 74% ee, respectively, when diazopyruvates 11 were used as substrates. The phenyliodonium ylide 7c yielded the adduct 8a in lower yield and poorer selectivity than the corresponding diazo precursor 7a (Table2) upon decomposition with [Ru(pybox)] catalysts. This suggests that ylide decomposition by RuII catalysts, contrary to that of the corresponding diazo precursors, does not lead to Ru-carbene complexes as reactive intermediates. Our method represents the first reproducible, enantioselective 1,3-cycloaddition of these types of substrates.
- Mueller, Paul,Chappellet, Sabrina
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p. 1010 - 1021
(2007/10/03)
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- SYNTHESIS OF α,β-EPOXY DIAZOMETHYL KETONES
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The preparation of eighteen epoxy diazomethyl ketones 1 is described.Two general methods were developed.Firstly, treatment of the mixed anhydrides of glycidic acids and carbonic acid ester with diazomethane led to the title compounds in yields ranging from 17-74 percent.Secondly, glycidyl chlorides which were obtained from sodium glycidates and oxalyl chloride, gave the desired products upon treatment with diazomethane ( yields 60-74 percent).The required α,β-epoxy carboxylic esters were prepared by Darzens condensation and epoxidation of α,β-unsaturated esters, but in some cases also by reaction of α-oxo carboxylic esters with diazomethane.
- Thijs, L.,Smeets, F. L. M.,Cillissen, P. J. M.,Harmsen, J.,Zwanenburg, B.
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p. 2141 - 2144
(2007/10/02)
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- 2-Acyl-3-substituted cyclopentan-1-ones and process for their preparation
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1,3-Dicarbonyl compounds useful as medicines, agricultural chemicals, perfumes, and their intermediates are prepared by reacting a specific α,β-unsaturated carbonyl compound with a specific organic copper lithium compound in the presence of an aprotic inert organic solvent, and then reacting the reaction product with an organic carboxylic acid halide or anhydride. In particular, novel 2-acyl-3-substituted cyclopentan-1-ones and 2-acyl-3-substituted cyclohexan-1-ones having important physiological activities are provided.
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