7 results about "Intramolecular reaction" patented technology

The present invention relates to a novel synthetic procedure utilizing domino Knoevenagel- cyclization reactions, in which the furan, thiophene or pyrrole subunits of the substrates undergo a Diels-Alder cycloaddition as either a diene or a dienophile producing novel condensed tetra- penta- or hexacycles with bridged or spirocyclic dihydrofuran, -thiophene or -pyrrole moiety. The five-membered aromatic heterocyclic subunit reacts intramolecularly as a diene with the double bond in a [4+2] or [4+4] cycloaddition (1,4-addition to five-membered heterocycle) producing bridged scaffolds. The cyclization step can also be an intramolecular hetero Diels- Alder reaction, in which a heterodiene reacts intramolecularly with the π-excessive five- membered heterocycles acting as a dienophile in the 1,2-addition. Some of the novel condensed heterocyclic products have antiproliferative activity and thus both the compounds and their therapeutic application are subject of the invention.

The invention discloses a silicon-containing conjugated olefin compound as well as a preparation method and application thereof, the structural formula of the silicon-containing conjugated olefin compound is shown as (I), and the silicon-containing conjugated olefin compound is obtained by carrying out silicon-carbon bond breakage synthesis on an allenyl functionalized silicon hybrid quaternary compound in the presence of a ligand, a palladium catalyst and a reaction medium, the allene functionalized silicon hybrid quaternary compound is used as a reactant to directly perform intramolecular reaction under the action of a complex formed by a metal catalyst and a phosphine ligand, the reaction condition is mild, the method is simple, and the obtained crude product can be purified by a silica gel rapid chromatography to obtain a pure product. The method has the advantages of mild reaction conditions, wide substrate expansion range, simple preparation operation and the like, and the prepared compound has a certain application prospect in the anti-tumor field.

The present invention relates to the technical field of herbicides, and provides an N,N-diacetyl-[1,4,5]oxadiazepane and a preparation method thereof. The method is obtained by reacting N,N-diacetylhydrazine with 2,2-dichlorodiethyl ether in the presence of a base, and specifically includes: further mixing a mixture composed of the N,N-diacetylhydrazine, the 2,2-dichlorodiethyl ether and a solvent with the base so that the mass concentration of the N,N-diacetylhydrazine in the reaction system is below 5% for reaction. The method of the present invention can promote more intramolecular reactions of reaction intermediates rather than intermolecular reactions, improve the selectivity of the reaction, and improve the yield of N,N-diacetyl-[1,4,5]oxadiazepane.

The application discloses a synthesis method of Triclabendazole, which comprises the following steps: starting from a compound of formula (11) and a compound of formula (10), a Pictet-Spengler reaction is performed, then intermolecular aldol condensation of a compound of formula (8) and a compound of formula (14) is performed, a fragment connection product of formula (15) is obtained through the reaction, then asymmetric ketal oxidation is performed to obtain a compound of formula (19-II), an intramolecular Stecker reaction is performed to obtain a compound of formula (5), then stereoselective decarboxylation protonation of palladium catalysis is performed to obtain a compound of formula (3), then a protecting group is removed, and an ethyl ester is reduced to obtain a compound of formula (26); then, the Triclabendazole shown in formula (A) is synthesized from the compound of formula (26). The method is mild in conditions, simple in operation, and raw materials are easy to obtain, and is suitable for large-scale production.

This invention provides a 2,3-dihydrobenzo[d][1,3]oxaphosphazene derivative of formula (I) and its preparation method. Compound I is constructed by tandem nucleophilic addition (or nucleophilic substitution) and intramolecular S-NAr reaction. This method features simple preparation steps, high yield, and mild reaction conditions, solving the technical problems of complex synthesis steps and harsh conditions in the synthesis of oxaphosphine compounds in traditional prior art.

The invention provides a benzoxadiketone compound and a preparation method thereof, and belongs to the technical field of organic synthesis. The preparation method comprises the following steps: mixing 2-aryl vinyl sulfonyl fluoride serving as a raw material with high phthalic anhydride containing different functional group substituted phenyl groups, carrying out a simple Michael addition reaction, carrying out an intramolecular cyclization reaction under the action of alkali, and further carrying out an intramolecular SN2 reaction to obtain a benzoxadiketone compound; the benzoxadione compound possibly has certain biological activity and has a potential medicinal prospect; the preparation method has the advantages of mild reaction conditions, wide substrate application range, low requirements on instruments and equipment, simple operation, good yield, simple and easily available raw materials, and good practicability.

The invention provides a preparation method of an AT-406 intermediate, and belongs to the technical field of medical intermediates. According to the method, methyl L-pyroglutamate is subjected to ethynylation, and a selected ester solvent and a hydroboration reagent are subjected to hydroboration reductive amination reaction, so that the reaction selectivity can be improved, isomer impurities are reduced, separation and purification are easy, a single cis-configuration product can be obtained, and the ee value can reach 99.5% or above. The specific hydroboration reagent and the oxidation reagent are selected, so that the use of ozone and reagents with strong mercaptan odor is avoided, the selectivity of intramolecular reaction is improved, the generation of byproducts is reduced, separation and purification are easy, the catalyst and the byproducts are non-toxic and pollution-free to the environment, and the method is suitable for industrial production. The invention provides a method suitable for industrial production to obtain the AT-406 intermediate.