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• 57097-81-1 3-bromo-5-methyl-1H-pyrazole 

Relevant academic research and scientific papers

NITROGEN-CONTAINING FUSED BICYCLIC COMPOUNDS AND THEIR USE AS UBIQUITIN-SPECIFIC-PROCESSING PROTEASE 1 (USP1) INHIBITORS

The present disclosure provides compounds having Formula (I): (I) and the pharmaceutically acceptable salts and solvates thereof, wherein X1, X2, X3, X4, X5, X6, X7, X8, R1, R2, R6, R6', R7, and R7' are defined as set forth in the specification. The present disclosure is also directed to the use of compounds of Formula (I) to inhibit a USP1 protein and/or to treat a disorder responsive to the inhibition of USP1 proteins and USP1 activity. Compounds of the present disclosure are especially useful for treating cancer.

Preparation method of chlorantraniliprole intermediate

The invention discloses a preparation method of a chlorantraniliprole intermediate and belongs to the technical field of agricultural pesticides. The preparation method of the chlorantraniliprole intermediate comprises the following steps of dropwise adding ethyl diazoacetate into ethyl acrylate, which serves as reaction reagent and solvent, to obtain a compound I; at room temperature mixing and overnight standing the compound 1 and 4-methoxybenzyl chloride inside a potassium carbonate medium to obtain a compound 2; hydrolyzing the compound 2 in alkaline reagent to regulate the PH to obtain acompound 3; reacting the compound 3 with excessive NBS (N-bromosuccinimide) to obtain a compound 4; refluxing the compound 4 inside a trifluoroacetic acid medium for reaction to obtain a compound 5; subjecting the compound 5 and 2, 3-dichloropyridine to low-temperature reaction inside a sodium ethoxide medium to obtain a compound TM. The preparation method of the chlorantraniliprole intermediate is concise in technical processes, cheap and simple in acquisition of raw materials, mild in reaction conditions, simple in operation and applicable to industrial production and has the advantages of being simple and practical, high in economic efficiency and yield, few in side reaction and low in environmental pollution.

A synthesis method of chlorine insect benzamide (by machine translation)

The present invention discloses one kind of chlorine insect benzamide synthesis method, relates to the field of organic synthesis. The invention two key intermediate 1 - (3 - chloro - 2 - pyridyl) - 3 - bromo - 1 H - 5 - pyrazole carboxylic acid with N - methyl - 3 - methyl - 2 - amino - 5 - chloro - benzamide synthesis method to re-design and improvement. Finally through the amidation reaction synthesize a final product chlorine insect benzamide. The synthesizing method of the invention for the intermediate 1 - (3 - chloro - 2 - pyridyl) - 3 - bromo - 1 H - 5 - pyrazole carboxylic acid synthesis provides a path; in the synthesis method steps of mild reaction conditions, and the steps can get better yield, overcomes the harsh reaction conditions in the prior art, the key steps to the problem of low yield, greatly reduces the production cost of the chlorine insect benzamide; in this synthetic method, the various steps in the few by-products, easy separation and purification, to further facilitate the industrial production. (by machine translation)

Intermediate 1 - (3 - chloro - 2 - pyridyl) - 3 - bromo - 1H - 5 - pyrazolyl formic acid

Relating to the organic synthesis field, the invention in particular discloses a synthesis method for an intermediate 1-(3-chloro-2-pyridyl)-3-bromo-1H-5-pyrazolecarboxylic acid. The synthesis method includes the steps of: taking 3-aminocrotononitrile as the raw material, mixing the raw material with hydrazine hydrate, carrying out cyclization reaction, bromination reaction, oxidation reaction and condensation reaction in order to obtain 1-(3-chloro-2-pyridyl)-3-bromo-1H-5-pyrazolecarboxylic acid. The synthesis method provided by the invention provides a path for synthesis of the intermediate 1-(3-chloro-2-pyridyl)-3-bromo-1H-5-pyrazolecarboxylic acid, the reaction conditions of each step are mild, good yield can be achieved, and the production cost is reduced.