Preparation method of 2-(2-(tert-butyloxycarbonyl)-2-azaspiro [3.4] octane-5-yl) acetic acid

A technology of butoxycarbonyl and azaspiro, which is applied in the field of compound synthesis, can solve the problems of no literature reports on the synthesis method, and achieve the effects of reasonable reaction process design, easy reaction and short route
CN112552222AActive Publication Date: 2021-03-26南通药明康德医药科技有限公司
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
南通药明康德医药科技有限公司
Publication Date
2021-03-26

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Abstract

The invention discloses a preparation method of 2-(2-(tert-butyloxycarbonyl)-2-azaspiro [3.4] octane-5-yl) acetic acid. The preparation method comprises the following steps: dissolving a compound 1 and a compound 2 in 2-methyl tetrahydrofuran, dropwise adding lithium bis (trimethylsilyl) amide, and reacting to obtain a compound 3; dissolving the compound 3 into acetone, and reacting with sodium iodide to obtain a compound 4; dissolving the compound 4 in 2-methyl tetrahydrofuran, dropwise adding n-butyllithium, and reacting to obtain a compound 5; dissolving the compound 5 into 2-methyl tetrahydrofuran, then adding a compound 6, alkali and 1, 8-diazabicyclo undecene-7-ene, and reacting at room temperature to obtain a compound 7; dissolving the compound 7 into ethyl acetate, adding a catalyst, and reacting in hydrogen to obtain a compound 8; dissolving the compound 8 into tetrahydrofuran and water, adding alkali for hydrolysis to obtain a final compound 9, and continuously optimizing thestructure of a spiro compound to obtain the synthesis method suitable for industrial production.
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Description

technical field

[0001] The invention relates to a compound synthesis method, in particular to a compound 2-(2-(tert-butoxycarbonyl)-2-azaspiro[3.4]octane-5-yl)acetic acid preparation method. Background technique

[0002] Compared with foreign competitors, Chinese pharmaceutical companies are often plagued by technical and financial problems, unable to effectively carry out new drug research and development, and can only simply repeat the production or imitate foreign patent expired drugs. The products lack international competitiveness, and the domestic market also suffers. The serious threat of imported western medicines, and the discovery of lead compounds is the only way to discover innovative drugs. Due to the long cycle of new drug development (8-10 years) and high cost (800-100 million US dollars), most developed countries currently adopt the method of "many, fast, high, and low cost"—combinatorial chemical technology platform to speed up the development of small molec...

Claims

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