Industrial production method of atazanavir intermediate tert-butyl 2-[4-(2-pyridyl)benzyl]-carbazate

The invention relates to the technical field of biological industry, in particular to an industrial production method of atazanavir intermediate tert-butyl 2-[4-(2-pyridyl)benzyl]-carbazate. The industrial production method includes: subjecting p-chlorobenzaldehyde as a raw material to aldolization,...

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Bibliographische Detailangaben
Hauptverfasser: XU JING, ZHONG CHONGCHAO, WANG YUQIN
Format: Patent
Sprache:chi ; eng
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Zusammenfassung:The invention relates to the technical field of biological industry, in particular to an industrial production method of atazanavir intermediate tert-butyl 2-[4-(2-pyridyl)benzyl]-carbazate. The industrial production method includes: subjecting p-chlorobenzaldehyde as a raw material to aldolization, carrying out Grignard coupling reaction, carrying out reductive amination to generate phenylhydrazone, and carrying out hydrogenation to obtain the target product tert-butyl 2-[4-(2-pyridyl)benzyl]-carbazate. Compared with the prior art, the industrial production method has the advantages of high efficiency, good stability, low cost, good operational convenience and the like, and is suitable for continuous production of high-quality products, with product purity reaching 99% and above and unknow impurity content less than 0.3%. 本发明涉及生物化工技术领域,具体涉及阿扎那韦关键中间体2-[4-(2-吡啶基)苄基]-肼羧酸叔丁酯工业化生产方法,以对氯苯甲醛为原料,经过缩醛反应、格氏偶联反应、还原氨化生成苯腙、再经过氢化反应得到目标产品2-[4-(2-吡啶基)苄基]-肼羧酸叔丁酯。与现有的工艺比较,具有高效、稳定、成本较低、易操作等特点,可连续生产高品质产品,产品纯度达到99%以上,未知单杂小于0.3%。