1036931-35-7Relevant articles and documents
N - benzyl -4 - cyclobutyl -2 - hydroxy -3 - nitryl Ding amide and use thereof
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Paragraph 0031; 0046-0053, (2017/07/14)
The invention relates to a new compound, and in particular relates to N-benzyl-4-cyclobutyl-2-hydroxy-3-nitrobutyrylamide and use thereof, and belongs to the technical field of the preparation of medicine and other fine chemical products. The structural formula of the N-benzyl-4-cyclobutyl-2-hydroxy-3-nitrobutyrylamide is shown in the specification; the compound is used for synthesizing beta-amino-alpha-hydroxy cyclobutane butyrylamide hydrochloride (formula I). According to the preparation method of N-benzyl-4-cyclobutyl-2-hydroxy-3-nitrobutyrylamide, the raw materials 2-nitroethyl cyclobutane (formula III) and N-benzyl-2-oxoacetamide (formula IV) are condensed in an alkaline environment in the presence of an organic solvent to obtain N-benzyl-4-cyclobutyl-2-hydroxy-3-nitrobutyrylamide.
A intermediate pope Switzerland Wei 2-hydroxy-3-amino-4-cyclobutyl butanamide hydrochloride synthetic method
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Paragraph 0037; 0041, (2017/02/28)
The invention relates to a synthetic method of a boceprevir intermediate namely 2-hydroxy-3-amino-4-cyclobutane amide hydrochloride, belonging to the technical field of medicament synthesis. By adopting the synthetic method, the problems that a method for synthesizing the boceprevir intermediate is high in cost, complex in reaction, low in efficiency and the like in the prior art can be solved. The synthetic method comprises the following steps: by adopting cyclobutyl acetate and monomethyl mono potassium malonate as raw materials, reacting for 10-12 hours at room temperature under the action of an activating agent and magnesium chloride; sequentially adding an oxidizing agent, 4-cyclobutyl-3-oxo-ethyl butyrate and a catalyst into methanoic acid at 15-20 DEG C, and reacting for 1.5-2.5 hours at 15-20 DEG C; adding a condensation agent and organic alkali at 10-15 DEG C, performing condensation reaction with ammonium chloride at room temperature, and reacting for 10-12 hours; and finally performing ammoniation and acidification to obtain a final product. The synthetic method disclosed by the invention is relatively low in cost, simple in reaction condition, less in reaction step and short in time, and the final product, namely the boceprevir intermediate, is relatively high in purity and yield.
PROCESS FOR PREPARATION OF BOCEPREVIR AND INTERMEDIATES THEREOF
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Page/Page column 9; 37-38, (2014/05/07)
THE PRESENT INVENTION RELATES TO AN IMPROVED PROCESS FOR THE PREPARATION OF (1R,5S)-N-[3-AMINO-1-(CYCLOBUTYLMETHYL)-2,3-DIOXOPROPYL]-3-[2(S)-[[[(1,1-DIMETHYLETHYL)AMINO]CARBONYL] AMINO]-3,3-DIMETHYL-1-OXOBUTYL]-6,6-DIMETHYL-3-AZABICYCLO[3.1.0]HEXAN-2(S)-CARBOXAMIDE AND ITS INTERMEDIATES