Preparation method of fodor stanozolol suitable for industrialized production

Abstract

The invention relates to a preparation method of fodor stanozolol suitable for industrialized production. According to the preparation method disclosed by the invention, water-ethanol is used as a reaction solvent, amine substances are used as a catalyst, after the reaction is completed, temperature reduction and crystallization are performed, and products are separated in a precipitation form. The whole process is easy to control and high in repeatability, the yield of the fodor stanozolol is stabilized to 95%, and the residue quantity is controlled within 0.05%, so that medical standards are completely met, and the preparation method is very suitable for industrialized production.

Description

technical field [0001] The invention relates to the preparation of fudosteine, an antitussive and phlegm-reducing drug, and belongs to the technical field of medicine. Background technique [0002] Fudosteine ​​(chemical name: 3-hydroxypropylthioalanine) is a class of compounds with the basic skeleton of steine ​​developed by Japan SSP Pharmaceutical Co., Ltd. in 1988. It was first introduced in October 2001 Listed in Japan. Pharmacological experiments have proved that it has many functions such as inhibiting goblet cell hyperplasia, promoting serous tracheal secretion and inhibiting tracheal inflammation. Due to its strong efficacy, small side effects, wide indications and great market potential, fudosteine ​​is expected to become Alternative products of similar drugs. [0003] The synthetic method of this compound is mainly divided into two classes at present: [0004] One method is the reaction of L-cysteine ​​and allyl alcohol under the action of light, microwave, hea...

AI Technical Summary

Problems solved by technology

[0009] The biggest disadvantage of this method is that it is difficult to remove the inorganic salts in the final product, which easily leads to high residue

For example, US5047428 has reported that L-cysteine ​​and 3-bromo-1-propanol react to prepare fudosteine. The method has a long reaction time, and the reaction process can produce equimolar inorganic salts, and fudosteine ​​is soluble in water. , insoluble in organic solvents, it is not easy to remove inorganic salts from the product, resulting in high product residues, which is not conducive to industrial production; Chinese patent application 200910167947.0 reported the reaction of L-cysteine ​​and 3-chloro-1-propanol to prepare Fodos Fudosteine, using the solubility difference between fudosteine ​​and sodium chloride to purify fudosteine, but the experimental process requires hot filtration (≥95°C), the steps are cumbersome, the operation is complicated, and the product will be more lost

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