Process for preparing butylphthalide
A preparation process, the technology of butylphthalide, which is applied in the field of new preparation technology of butylphthalide, can solve the problems that the process is not suitable for industrial production, and achieve the effect of simple operation
Active Publication Date: 2019-08-16
福建省宝诺医药研发有限公司
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[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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[0023] 1. Preparation of butylphthalide
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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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Patent Type & Authority Patents(China)
IPC IPC(8): C07D307/88
CPCC07D307/88
Inventor 邱小龙胡林邹平储玲玲王虎王平时光好张新刚沈伟彭陟辉张义森王东辉游正伟
Owner 福建省宝诺医药研发有限公司
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