8 results about "Radical cyclization" patented technology

The invention provides indole C3-O functionalized derivatives as well as a preparation method and insecticidal and antibacterial application thereof, and relates to the technical field of pesticide development. The indole C3-O functionalized derivative provided by the invention has a structure of a general formula (1), is prepared through a free radical cyclization reaction catalyzed by N-heterocyclic carbene (NHC), does not need a transition metal catalyst, and efficiently constructs a C3-site oxygen functional group by taking o-nitroalkyne or cis-o-nitrostyrene and aldehyde as raw materials through multi-step series conversion in an inert atmosphere. The method has the advantages of being high in atom economy, good in functional group compatibility, easy and convenient to operate, environmentally friendly and the like. The obtained derivative shows remarkable activity in prevention and treatment of various agricultural diseases and insect pests such as rice sheath blight disease, aflatoxin and brown planthopper, can be prepared into various pesticide preparations, has the characteristics of broad spectrum, high efficiency and low toxicity, and is suitable for development of green pesticides.

The invention discloses a method for preparing a polyfluoroalkyl coumarin derivative, and belongs to the field of organic synthesis. According to the method, cheap and easily available polyfluorocarboxylic acid anhydride is used as a polyfluoroalkylating reagent, and in-situ activation of NHPI is combined to prepare the C3-site polyfluoroalkyl substituted coumarin derivative. Under the condition of visible light catalysis, polyfluoroalkyl carboxylic acid anhydride is used as a polyfluoroalkylating reagent, polyfluoroalkyl free radicals are generated through in-situ activation of NHPI, the free radicals and aromatic propiolate are subjected to a free radical cyclization rearrangement reaction, and finally preparation of the C3-site polyfluoroalkyl substituted coumarin derivative is achieved. The polyfluoroalkyl carboxylic acid anhydride used in the method is stable in property, low in price and easy to obtain, and the synthesis cost is reduced. The method is wide in applicable substrate range and applicable to various polyfluoroalkyl carboxylic acid anhydrides, and the tolerance of reaction functional groups is good.

This invention discloses a method for synthesizing trifluoromethylated polycyclic indole derivatives using visible light photocatalysis, belonging to the field of organic synthesis technology. This invention is the first to disclose a method for synthesizing trifluoromethylated polycyclic indole derivatives under visible light photocatalysis via CF3Br and... N This invention relates to a method for the one-step preparation of trifluoromethylated polycyclic indole derivatives, namely 2,3-dihydropyrrolo[1,2-a]indole and 5,6-dihydroindole[2,1-a]isoquinoline derivatives, through a free radical cyclization reaction of alkenyl indole derivatives. This invention is the first to use CF3Br as a trifluoromethylating agent, via CF3Br reacting with... N The radical cyclization reaction of α-alkenyl indole derivatives successfully constructed trifluoromethylated 2,3-dihydropyrrole[1,2-a]indole and 5,6-dihydroindole[2,1-a]isoquinoline derivatives. Compared with other trifluoromethylating reagents used in the prior art, CF3Br has the advantages of low cost, easy availability and high atom utilization. Compared with the existing synthetic methods, the method provided by this invention greatly reduces the synthesis cost and has a high possibility of large-scale production.

The application discloses a novel method for preparing an intermediate of an aryl abietane diterpene Plebein C, and specifically comprises the following steps: substituting a carbonyl alpha position of 4,4-dimethyl-2-cyclohexen-1-ketone to obtain compound I; protecting the compound I by TBS to obtain compound II; performing a Luche reduction reaction on the compound II to obtain compound III; performing an iodination reaction on 3-hydroxy-4-methoxybenzaldehyde to obtain compound IV; performing a Wittig reaction on the compound IV to obtain compound V; performing a Mitsunobu reaction between the compound III and the compound V to obtain compound VI; performing a radical cyclization reaction on the compound VI to obtain compound VII; performing an oxidation on a benzyl position of the compound VII to obtain compound VIII; and finally performing an oxidation and a ring closure on the compound VIII to obtain a five-ring intermediate compound IX of a Plebein C molecule; the preparation method has the advantages of simple synthetic route, low-cost and easily-obtained reagents, high yield, favorability for industrial preparation of the intermediate, and strong popularization potential.

The invention provides a synthesis method of beraprost. The synthesis method comprises the following steps: step a), preparing a compound 39 from a compound 30 and a compound 31; step b), preparing a compound 10 from a compound 02 and the compound 39 through a free radical cyclization reaction; and step c): taking the compound 10 as a raw material, and carrying out reduction reaction, deprotection, column chromatography and hydrolysis to obtain a beprostaglandin compound 14. The preparation method disclosed by the invention utilizes the free radical cyclization reaction participated by an organic tin reagent, and realizes efficient and simple synthesis of beprostaglandin with short route and simple operation through a convergent route.

The invention belongs to the technical field of compound synthesis, and particularly relates to the technical field of synthesis of dihydropyridazine derivatives. The invention discloses a method for synthesizing a 5, 6-dihydropyridazine derivative by utilizing a free radical cyclization reaction promoted by visible light, which is characterized in that (E)-N '-benzylidene-N-(butyl-3-ene-1-yl) acethydrazide derivative and sodium trifluoromethanesulfinate react in a solvent under the conditions of a photocatalyst and light irradiation to obtain a product. The method is carried out under mild conditions, the reaction system is simple, the method selectivity and yield are high, no other complex by-products are generated, and high purity is easy to achieve; the substrate is wide in application range and good in functional group tolerance; byproducts are few, and energy consumption is low. According to the method, visible light catalysis is adopted, free radical cyclization is achieved, sodium trifluoromethanesulfinate is used as a starting material, dimethyl sulfoxide is used as a solvent system, the reaction condition is simple, and the reaction efficiency is high.

The present disclosure provides methods of synthesizing a compound of Formula I. The method proceeds through several different pathways including a radical cyclization. Also disclosed are compositions the compound of Formula I as well as methods of using the compound of Formula I in the treatment several conditions or disorders.

The present disclosure provides methods of synthesizing a compound of Formula I. The method proceeds through several different pathways including a radical cyclization. Also disclosed are compositions the compound of Formula I as well as methods of using the compound of Formula I in the treatment several conditions or disorders.