- Radical Carbonyl Propargylation by Dual Catalysis
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Carbonyl propargylation has been established as a valuable tool in the realm of carbon–carbon bond forming reactions. The 1,3-enyne moiety has been recognized as an alternative pronucleophile in the above transformation through an ionic mechanism. Herein, we report for the first time, the radical carbonyl propargylation through dual chromium/photoredox catalysis. A library of valuable homopropargylic alcohols bearing all-carbon quaternary centers could be obtained by a catalytic radical three-component coupling of 1,3-enynes, aldehydes and suitable radical precursors (41 examples). This redox-neutral multi-component reaction occurs under very mild conditions and shows high functional group tolerance. Remarkably, bench-stable, non-toxic, and inexpensive CrCl3 could be employed as a chromium source. Preliminary mechanistic investigations suggest a radical-polar crossover mechanism, which offers a complementary and novel approach towards the preparation of valuable synthetic architectures from simple chemicals.
- Huang, Huan-Ming,Bellotti, Peter,Daniliuc, Constantin G.,Glorius, Frank
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supporting information
p. 2464 - 2471
(2020/12/07)
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- Synthesis method of propyzamide based on oxidation reaction
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The invention discloses a novel synthesis method of propyzamide. The method is characterized in that cheap dichlorobenzoic acid is used as a raw material. According to the method, the propyzamide product can be obtained without a complex reaction with harsh conditions and high toxicity and without using a high-activity, expensive and environment-harmful reagent. Compared with an existing synthesis method, the method has the advantage that high-activity acyl chloride reagents and expensive and easily degradable alkynyl amine substances are avoided. The method is integrally simple in route, economical, environment-friendly, safe and efficient, and has high industrial application potential.
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Paragraph 0014
(2021/09/21)
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- NURR1 RECEPTOR MODULATORS
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Described herein, inter alia, are Nurr1 receptor modulators and uses thereof. In an aspect is provided a method for treating a disease associated with dysregulation and/or degeneration of dopaminergic neurons in the central nervous system of a subject in need thereof, the method including administering to the subject in need thereof a therapeutically effective amount of a compound described herein.
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Paragraph 0646; 1971-1973
(2020/09/08)
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- Preparation method for propyzamide
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The invention discloses a preparation method for propyzamide. The preparation method comprises the following steps: preparing 3-chloro-3-methylbutyne through a chlorination reaction; then preparing 3-amino-3-methylbutyne through an aminolysis reaction; and then carrying out an amidation reaction so as to prepare high-purity propyzamide. The optimal preparation method for propyzamide is screened out through a large number of experiments; the preparation method is reasonable in the whole process design and simple and efficient in process operation; in particular, optimal reaction conditions arescreened out, optimal raw material composition is determined for the chlorination reaction in the step 1, the aminolysis reaction in the step 2 and the amidation reaction in the step 3, and the proportions of reaction raw materials, reaction temperature, reaction time and the like are optimized, so reaction yield can be greatly increased (wherein the yield can reach 93% or more), side reactions can be reduced, reaction rate can be increased, and production cost can be greatly lowered; so the preparation method has good application prospects.
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- A method for preparing alkyne benzoyl grass amine (by machine translation)
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The present invention provides a method for preparing alkyne benzoyl grass amine, comprising a condensation step: by parts by mass to 3 - amino - 3 - methyl [...] 100 - 105 parts, triethylamine 2 - 5 parts and solvent 100 - 500 parts into 10% -32% ω of sodium hydroxide solution 200 - 400 parts by, after stir, dropping 3, 5 - dichloro benzoyl chloride 100 - 105 parts, temperature control in 12 - 15 °C, after dropping, thermal insulation 1 - 5 hours. The alkyne benzoyl grass amine preparation method of the advantage of high purity of the product. (by machine translation)
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- Palladium-Catalyzed Cascade Difluoroalkylation/Cyclization of N-Propargylamides: Synthesis of Oxazoles and Oxazolines
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A palladium-catalyzed process to construct oxazoles and oxazolines with broad functional-group tolerance has been developed, and the method introduces difluoromethyl groups into heterocycles in a one-pot fashion. This system uses a carbonyl oxygen as the acceptor for the addition of a vinylpalladium intermediate to achieve the cyclization. Oxazoline derivatives are generated as the Z-isomer with high stereoselectivity. Additionally, we validated the tentative mechanism of this reaction.
- Ma, Jun-Wei,Wang, Qiang,Wang, Xin-Gang,Liang, Yong-Min
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p. 13296 - 13307
(2018/11/02)
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- NOXIOUS ARTHROPOD CONTROL AGENT CONTAINING AMIDE COMPOUND
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An object of the present invention is to provide a compound having the controlling activity on a noxious arthropod, and a noxious arthropod controlling agent containing an amide compound of formula (I): wherein X represents a nitrogen atom or a CH group, p represents 0 or 1, A represents a tetrahydrofuranyl group or the like, R1, R2, R3, R4, R5, R6 and R7 represent a hydrogen atom or the like, n represents 1 or 2, Y represents an oxygen atom or the like, m represents any integer of 0 to 7, and Q represents a C1-8 chain hydrocarbon group optionally having a phenyl group or the like, has the excellent noxious arthropod controlling effect.
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- Preparation method of propyzamide
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The invention relates to an organic synthesis method and in particular relates to a preparation method of propyzamide. According to the method provided by the invention, 3,5-dichlorobenzeneformonitrile is used as a raw material, and is subjected to alcoholysis reaction with 3-methyl-3-hydroxybutyne under a Lewis acid catalytic condition to synthesize the propyzamide in one step. With the adoption of the preparation method of the propyzamide, a process path is simplified, reaction conditions are improved and the yield of a product is improved; the emission of three wastes is greatly reduced, and a green and feasible scheme is provided for industrial production.
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Paragraph 0003
(2016/10/09)
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- Development of a process for triazine-promoted amidation of carboxylic acids
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A process has been developed for the triazine-promoted amidation of carboxylic acids. We have identified 2,4,6-trichloro-1,3,5-triazine (cyanuric chloride) as a cost-effective reagent for this transformation. The procedure is a suitable alternative to traditional amidation processes when an acid chloride cannot be prepared from the corresponding carboxylic acid due to safety, stability, or handling concerns.
- Rayle, Heather L.,Fellmeth, Lisa
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p. 172 - 176
(2013/09/08)
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- Process of improving activity of herbicides and fertilizers using N-(2-hydroxyethyl)-acetamide or -propanamide
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The invention is related to the use of certain water-soluble compounds known as such and having the Formula for the modulation of membrane dependent metabolism processes within living cells, in particular with relation to transport phenomena and cell procedures which are induced or influenced by active agents supplied from outside the cell, products containing these substances for the above described uses and processes using these products.
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- 5,6-Dihydro-1,2,4,6-thiatriazin-5-one-1,1-dioxides
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5,6-Dihydro-1,2,4,6-thiatriazin-5-one-1,1-dioxides of the formula STR1 where R1 is hydrogen, a metal atom or an unsubstituted or substituted ammonium radical, R2 is a saturated or unsaturated straight-chain aliphatic radical of up to 10 carbon atoms, a cycloaliphatic radical or 3 to 7 carbon atoms, a branched saturated or unsaturated aliphatic radical of 3 to 10 carbon atoms, a halogen-, alkoxy- or alkylmercapto-substituted aliphatic radical of 2 to 10 carbon atoms tetrahydrofuryl substituted methyl, a cycloalkoxy-substituted aliphatic radical of 4 to 10 carbon atoms, unsubstituted or halogen-substituted benzyl or phenyl, halophenyl, or alkylphenyl of a total of up to 10 carbon atoms, R3 is hydrogen, a straight-chain aliphatic radical of up to 10 carbon atoms, a cycloaliphatic radical of 3 to 7 carbon atoms, a branched aliphatic radical of 3 to 10 carbon atoms, haloalkyl, or alkoxyalkyl of 2 to 10 carbon atoms and X is oxygen and may also be sulfur if R2 is unsubstituted or halogen-substituted benzyl, processes for their preparation, and herbicides containing the above compounds.
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