Synthesis method of 5, 7-dichloro-1, 2, 3, 4-tetrahydroisoquinoline hydrochloride

The invention relates to a synthesis method of 5, 7-dichloro-1, 2, 3, 4-tetrahydroisoquinoline hydrochloride, and belongs to the technical field of synthesis of medical intermediates. The method comprises the steps that 3, 5-dichlorobenzaldehyde serves as a raw material, 5, 7-dichloro-1, 2, 3, 4-tet...

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Hauptverfasser: NIU XIAODONG, ZHENG GUANGBING, GUO KAI, LI JIAN
Format: Patent
Sprache:chi ; eng
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Zusammenfassung:The invention relates to a synthesis method of 5, 7-dichloro-1, 2, 3, 4-tetrahydroisoquinoline hydrochloride, and belongs to the technical field of synthesis of medical intermediates. The method comprises the steps that 3, 5-dichlorobenzaldehyde serves as a raw material, 5, 7-dichloro-1, 2, 3, 4-tetrahydroisoquinoline hydrochloride is obtained through Schiff base preparation, reduction, ring closing and reductive acidification reaction, and the total yield is 60% or above. The method avoids using expensive raw materials, and is simple in process route, mild in condition, low in production costand suitable for industrial production. 本发明涉及一种5,7-二氯-1,2,3,4-四氢异喹啉盐酸盐的合成方法,属于医药中间体合成技术领域。本发明所述的方法包括以3,5-二氯苯甲醛为原料,通过制备席夫碱、还原、关环及还原酸化反应得到5,7-二氯-1,2,3,4-四氢异喹啉盐酸盐,总收率在60%以上。本发明避免了使用昂贵的原料,且工艺路线简单,条件温和,生产成本低,适合工业化生产。