A kind of semi-synthetic method of high-purity and high-stability gastrodin

Abstract

The invention discloses a semi-synthesis method for high-purity and high-stability gastrodin. The semi-synthesis method comprises the following steps: carrying out a reduction reaction by taking tetraacethyl as a raw material; concentrating and adding a suitable amount of water into concentrated liquid; filtering and drying to obtain acethyl gastrodin; recycling a filtering solution which is used as a mother solution a; adding an alcohol solvent into the acethyl gastrodin to carry out a reflowing reaction, and concentrating; repeatedly reflowing and concentrating to obtain a concentrated solution; adding a non-polar solvent and filtering; drying solids to obtain a gastrodin rough product; recycling a filtering solution which is used as a mother solution b; adding alcohol and / or an ester solvent into the rough product of gastrodin; heating and completely dissolving; filtering and separating out crystals to obtain a refined product of gastrodin; recycling a filtering solution which is used as a mother solution c; mixing the mother solution b and the mother solution c; filtering and drying to obtain the rough product of gastrodin; and refining to obtain the refined product of gastrodin. The acethyl gastrodin prepared by the semi-synthesis method disclosed by the invention is stable, can be directly used as a crude drug, and can also be used as an intermediate to synthesize the high-purity gastrodin; the semi-synthesis method for the high-purity and high-stability gastrodin is very good for meeting the clinical demands on gastrodin and acethyl gastrodin.

Description

technical field [0001] The invention belongs to the technical field of drug synthesis, and in particular relates to a semi-synthetic method of gastrodin with high purity and high stability. Background technique [0002] Gastrodin is a natural compound and the core active ingredient of Gastrodia elata. Gastrodin has various physiological activities such as sedative, hypnotic, and anticonvulsant, and is mainly used clinically to treat dizziness, headache, deafness, tinnitus, and neurasthenia. In the late 1970s, Zhou Jun and others isolated a new compound from the traditional Chinese medicine Gastrodia elata, which was identified as 4-hydroxymethylphenyl-β-D-glucopyranoside. Pharmacological studies showed that this compound has sedative properties. , Hypnotic effect, considered to be the active ingredient of the traditional Chinese medicine Gastrodia elata, named gastrodin. In 1980, Zhou Jun and others completed the chemical synthesis of gastrodin, and after the continuous re...

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Problems solved by technology

However, Raney nickel or palladium charcoal has many disadvantages in the catalytic hydrogenation of catalysts: 1. The catalyst is expensive and the operations such as purchase and storage are troublesome. The recovery and reuse of the catalyst is also an extremely complicated matter, which brings difficulties for industrial continuous production. Pollution hazards caused by the surrounding environment; 2. Catalytic hydrogenation has special requirements for the reaction tank and the production site, and puts forward higher requirements for safe production, which virtually increases the cost of production management

The one-pot method of the prior art cannot directly separate the acetylgastrodin in the process, and the stability of the acetylgastrodin prepared by the reduction method is not good, which is very unfavorable for direct application or subsequent synthesis of gastrodin

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