Continuous synthesis method of olaparib
The invention discloses a continuous synthesis method of olaparib, which comprises the following steps: taking 2-fluoro-5-[(4-oxo-3, 4-dihydrophthalic acid-1-yl) methyl] benzoic acid as a raw material, sequentially carrying out acid activation reaction, selective monoacylation reaction and amidation...
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Format: | Patent |
Sprache: | chi ; eng |
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Zusammenfassung: | The invention discloses a continuous synthesis method of olaparib, which comprises the following steps: taking 2-fluoro-5-[(4-oxo-3, 4-dihydrophthalic acid-1-yl) methyl] benzoic acid as a raw material, sequentially carrying out acid activation reaction, selective monoacylation reaction and amidation reaction, and carrying out post-treatment to obtain the target product olaparib. Selective monoacylation of a piperazine ring is directly achieved through the condensing agent, piperazine amino does not need to be protected, reaction steps, consumption of reaction reagents and the like are reduced, the concept of low-carbon economy is met, continuous reaction is adopted in the whole reaction, efficient and green continuous production is achieved, the HPLC purity of the prepared pure olaparib product is 99% or above, and the purity of the pure olaparib product is higher than 99%. And preferably, the content is more than 99.6%.
本发明公开了一种奥拉帕尼的连续合成方法,包括如下步骤:以2-氟-5-[(4-氧代-3,4-二氢邻苯二甲酸-1-基)甲基]苯甲酸为原料,依次经酸活化反应、选择性单酰化反应、酰胺化反 |
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