Galanthamine intermediate compound V

A technology of galantamine and compound, applied in the field of galantamine intermediate compound V, can solve the problems of serious environmental pollution, high technical requirements and high production cost, achieve economical and environmental protection yield, high product purity and easy operation Effect
CN112521364APending Publication Date: 2021-03-19LUNAN PHARMA GROUP CORPORATION
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
LUNAN PHARMA GROUP CORPORATION
Publication Date
2021-03-19

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Abstract

The invention belongs to the field of pharmaceutical chemicals, and particularly relates to a galanthamine intermediate compound V. According to the invention, 4-(2-(methylamino)ethyl)phenyl acetate,paraformaldehyde and 1,3-benzodioxole are used as raw materials to synthesize the novel intermediate compound V. The invention also provides a novel method for synthesizing galanthamine by using the intermediate. According to the method, use of dangerous chemical reagents is avoided, the synthesized intermediate does not generate new impurities, a green catalyst is used for replacing a traditionalcatalyst, a reaction is milder, economical and environment-friendly, yield is higher, and the method is suitable for industrial production.
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Description

technical field

[0001] The invention belongs to the field of medicine and chemical industry, and in particular relates to a galantamine intermediate compound V. Background technique

[0002] Galanthamine, chemical name 11-methyl-3-methoxy-4a,5,9,10,11,12-hexahydro-6H-benzofuran-[3a,3,2ef] [2] Azepine-6-ol, molecular formula: C 17 h 21 NO 3 ; Molecular weight: 323.81; CAS registration number: 357-70-0, the structural formula is as follows:

[0003]

[0004] Galantamine was first researched and produced by Sopharma Pharmaceutical Company in Bulgaria, and its trade name is Nivalin. Pharmacological studies have proved that it is a potent inhibitor of acetylcholinesterase (AChE), and it also has a good regulatory effect on neuronal nicotinic receptors. It is widely used in the treatment of Alzheimer's disease ( Alzheimer's disease, AD) and myasthenia gravis and other diseases. At present, the drug has been launched in the United Kingdom, Ireland, the United States, China...

Claims

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