6 results about "Cycloheptatriene" patented technology

The application provides a preparation method and application of a compound III, and belongs to the field of medicinal chemistry. The method uses compound I as a raw material, and compound III is prepared through acyl chloride and Friedel-Crafts acylation reaction in a one-pot two-step method, and a reaction formula is shown in the following formula: The synthesis method provided by the application solves many pain points of the existing synthesis method using polyphosphoric acid as a dehydrating agent, for example, the polyphosphoric acid has strong corrosion, is viscous and not easy to transfer, the reaction temperature is high, the substrate is easy to polymerize, product purification needs vacuum distillation, and there are many phosphorus-containing waste water, etc. The synthesis method has the advantages of simple operation, environmental friendliness, mild and safe reaction conditions, high reaction yield and the like, and is suitable for large-scale production.

The application belongs to the technical field of medicine synthesis, and particularly relates to a 5H-dibenzo[a,d]cycloheptatriene-5-ketone intermediate compound and a method for preparing 5H-dibenzo[a,d]cycloheptatriene-5-ketone. The method uses SM-1 as a starting material, reacts with ethanethiol first, and then is coupled with SM-2 to obtain the intermediate compound I-2, and the compound I-2 can be reacted for one step under the action of a catalyst to obtain 5H-dibenzo[a,d]cycloheptatriene-5-ketone. The preparation method solves the problems of complex operation and high toxicity in the prior art, is simple to operate, the obtained product has high yield and purity, the reaction period is short, and is suitable for industrial production.

The application discloses a method for synthesizing a cycloheptatriene derivative by using DMAP as a catalyst, and the method comprises the following steps: using methyl coumarin and a gamma-substituted allene acid ester as raw materials, and performing a reaction in a solvent under the action of an organic base catalyst to synthesize the cycloheptatriene derivative in one step, wherein R 1 is any one of alkyl and a phenyl substituted by F, Cl, Br, Me and OMe. 2 R is any one of Et, Me, Bn and tBu. The synthesis method is simple to operate, raw materials and catalysts are simple and easy to obtain, reaction time is short, the scope of reaction substrates is wide, the yield of the target product is high, and the method has a wide industrial production prospect.

The preparation method comprises the following steps: carrying out dearomatization-ring expansion reaction on benzene under mediation of metals such as chromium to obtain a fluorinated cycloheptatriene complex; the preparation method comprises the following steps: carrying out a ligand dissociation-cyclization reaction on a fluoro cycloheptatriene complex to obtain 4-fluoro-4, 4a, 5, 5a, 6, 6a-hexahydro-1H-4, 6-vinylidene cyclopropyl [f] isobenzofuran-1, 3 (3aH)-diketone, and carrying out a ligand dissociation-cyclization reaction on the fluoro cycloheptatriene complex to obtain 4-fluoro-4, 4a, 5, 5a, 6, 6a-hexahydro-1H-4, 6-vinylidene cyclopropyl [f] isobenzofuran-1, the preparation method comprises the following steps: further carrying out condensation reaction on 4-fluoro-4, 4a, 5, 5a, 6, 6a-hexahydro-1H-4, 6-vinylidene cyclopropyl [f] isobenzofuran-1, 3 (3aH)-diketone to obtain the tecovirimat fluoro derivative. At normal temperature, the compound is a white solid, is easily soluble in methanol, ethanol and dichloromethane, and is slightly soluble in water. According to the method, starting from a cheap and easily available chemical product benzene, rapid construction of the tecovirimat fluoro derivative is realized, and the method has the advantages of mild reaction conditions, wide substrate application range, good selectivity, simple operation, easy product separation and the like. At 37 + / -5 DEG C, the solubility of the tecovirimat fluoro derivative VI in water is 8 [mu] g / mL, and compared with a tecovirimat drug, the solubility is obviously improved.

The application discloses a method for synthesizing a benzazepine derivative, which uses MBH carbonate and cycloheptatriene imine as raw materials, toluene as a solvent, heating to 80 DEG C, and one-step synthesis of a target product under the action of a commercial phosphine catalyst. 1 R is any one of Et, Me, tBu and Bn; R 2 is a phenyl or heteroaryl group substituted by any one of H, F, Cl, Me, OMe and NO2, 2-furyl, 2-quinolinyl and styryl; R 3 is any one of Me, 4-MeC6H5, 4-NO2C6H5 and 4-MeOC6H5. The synthesis method is simple in operation, simple in raw materials and catalyst, short in reaction time, wide in applicable range of reaction substrates, high in yield of the target product and wide in industrial production prospect.

The present application relates to a kind of visible light induced aromatic compound occurs to edit the reaction of de-aromatic skeleton to synthesize novel tricyclo [4,4,2,0] skeleton molecule method. Specifically under the action of photocatalyst, N-acetyl imine generates double radical, and through double radical iteration produces de-aromatic cycloheptatriene type double radical intermediate, then with alkyne occurs the radical type cycloaddition reaction. The present application obtains a series of novel tricyclo [4,4,2,0] skeleton molecules by simple and safe step.