Process for preparing butyphthalide

Abstract

The invention relates to a process for preparing butyphthalide. A one-pot method is adopted, the process is easy to operate, and industrial production has remarkable advantages. The process comprisesthe following steps: making 1,2-dibromo-benzene serving as an initial material react with carbon dioxide ice under the action of n-BuLi to generate an intermediate; directly adding n-BuLi into an intermediate solution without quenching the reaction; making the mixture react with n-valeraldehyde; treating a reaction liquid with HCl; and performing column chromatography and purification to obtain the butylphthalide.

Description

technical field [0001] The invention relates to a new process for preparing butylphthalide. Background technique [0002] Butylphthalide (also known as apigenin A, trade name Enbipu) is the third national class I anti-ischemic new drug with completely independent intellectual property rights and a brand-new chemical structure in China, and it is also the first in the world with the "deficiency" drug. Hemorrhagic stroke treatment" is a new chemical drug with the main indication. It has a single body structure with excellent safety, and has multiple pharmacological effects at the same time. It can comprehensively treat ischemic stroke, significantly reduce the loss of neurological function after infarction, and improve the living ability of patients. This compound was first discovered from the extract of southern water celery seed. It is mainly responsible for the aroma and taste of celery. After artificial chemical synthesis, the 3-position carbon atom in the chemical struct...

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Problems solved by technology

[0013] Although the above-mentioned method for preparing butylphthalide can successfully synthesize butylphthalide, the reported techniques are not suitable for industrial production

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