63876-32-4Relevant articles and documents
Preparation method of N-benzyl-3-oxopiperidine-4-carboxylic acid ethyl ester hydrochloride
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Paragraph 0018-0021; 0034-0037; 0042; 0044, (2020/02/10)
The invention provides a preparation method of N-benzyl-3-oxopiperidine-4-carboxylic acid ethyl ester hydrochloride, and the method comprises the following steps: (1) preparing an intermediate 2: dissolving N-benzyl glycine ethyl ester in an organic solvent, adding 4-halogenated ethyl butyrate and alkali, and reacting to obtain N-benzyl glycine ethyl ester; (2) dissolving the intermediate 2 in anorganic solvent, reacting with alkali, adjusting the pH value to 7-8 after the reaction is finished, adding water for washing, adjusting the pH value of an organic layer to 1-2, and separating out crystals to obtain a crude product; and (3) dissolving the crude product in water, adding alkali to adjust the pH value to 7-8, adding an organic solvent to extract, washing, adjusting the pH value of anorganic layer to 1-2, and crystallizing to obtain the product. The method is simple in process operation, high in product yield, high in purity and easy for industrial production.
With the biological activity of 5, 6, 7, 8 - tetrahydro-pyrido [3, 4 - d] pyrimidine compound and its preparation method and application (by machine translation)
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, (2017/08/02)
The invention discloses a has biological activity of 5, 6, 7, 8 - tetrahydro-pyrido [3, 4 - d] pyrimidine compound and its preparation method and application, which belongs to the with anti-tumor activity to the technical field of the synthesis of the compounds. The technical scheme of the present invention is to point: has biological activity of 5, 6, 7, 8 - tetrahydro-pyrido [3, 4 - d] pyrimidine compound, has the following structure:, wherein R1 For the ethyl carboxylic acid ester, ethylamine methyl, formyl methyl amine, dimethyl amino formyl, pyridine - 3 - methylene amino formyl, piperidine a acyl or anilino formyl, R2 For hydrogen or phenmethyl. The invention also discloses the has biological activity of 5, 6, 7, 8 - tetrahydro-pyrido [3, 4 - d] pyrimidine compound of preparation method and the preparation of anti-mammary tumor application of the medicament. The process of preparing the process is simple, easy to control, the target product high yield and good repeatability, prepared with anti-tumor activity of 5, 6, 7, 8 - tetrahydro-pyrido [3, 4 - d] pyrimidine compounds are all on breast cancer cell MCF - 7 has definite inhibitory effect. (by machine translation)
Preparation method for 1-benzyl-3-piperidone hydrochloride
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, (2017/03/08)
The invention discloses a preparation method for N-benzyl glycine ethyl ester. The method comprises the following steps: dissolving benzylamine in an organic solvent I, then adding 2-halogenated ethyl acetate, alkali and quaternary ammonium salt, and performing reaction to obtain the N-benzyl glycine ethyl ester. The invention also discloses a preparation method for 1-benzyl-3-piperidone hydrochloride. The method comprises the following specific steps: (1) preparing an intermediate IV (N-benzyl glycine ethyl ester); (2) dissolving the intermediate IV in an organic solvent II, then adding 4-halogenated ethyl acetate and alkali, and performing reaction to obtain an intermediate III; (3) performing reaction between the intermediate III and the alkali, reversely regulating a pH value to 6-8, performing concentration under reduced pressure, extracting by using ethyl acetate, performing washing and drying, and then performing concentration under reduced pressure to obtain an intermediate II; (4) performing reaction on the intermediate II and acid, performing rotary evaporation concentration, and adding a crystal solvent for crystallization to obtain a product. The route synthesis steps are short, the process is novel, the intermediates are high in purity, the product yield is high, and the cost is low.
