Synthesis method of apronal

A technology of valproic acid urea and synthesis method, which is applied in chemical instruments and methods, preparation of urea derivatives, preparation of organic compounds, etc., can solve the problems of using many kinds of raw materials, consuming more energy, increasing costs, etc., and achieve the synthesis route Simple and efficient, low cost and high raw material utilization
CN107501129AInactive Publication Date: 2017-12-22SHAANXI NORMAL UNIV
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
SHAANXI NORMAL UNIV
Publication Date
2017-12-22
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention discloses a synthesis method of apronal. The synthesis method takes isopentanoic acid or isopentanoate which is commercially cheap and available as a synthesis raw material and comprises the following steps: enabling the synthesis raw material and allyl bromide to react under an alkaline condition to generate 2-isopropyl-4-pentenoic acid or 2-isopropyl-4-pentanoate; hydrolyzing the 2-isopropyl-4-pentanoate under the alkaline condition to generate the 2-isopropyl-4-pentenoic acid; then transforming the 2-isopropyl-4-pentenoic acid into acyl chloride and enabling the acyl chloride to react with urea to obtain the apronal. According to the synthesis method disclosed by the invention, a synthesis route can realize medium-scale preparation of the apronal, with the need of two-step or three-step chemical transformation; the whole synthesis route is simple and efficient, simple and convenient to operate, low in cost and high in yield so that the synthesis method is suitable for large-quantity synthesis of the apronal.
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Description

technical field

[0001] The invention belongs to the technical field of medicine synthesis, and in particular relates to a synthesis method of valproic acid urea. Background technique

[0002] Valproylurea is a hypnotic / sedative drug. In 1926, the compound was synthesized by Hoffman-Roche Company and is known to the world under the trade name of "Sizionide". At the same time, valproic acid urea is also used as a general drug buffer, and is widely used clinically as a hypnotic drug.

[0003] In 1948, valproic acid urea was named "propylallyl acetylurea" in "Japanese Quasi-Pharmacopoeia" (third revision). In 2003, the SG compound granules with antipyretic and pain-relieving effects launched by Shionogi Pharmaceutical Company of Japan contain this ingredient. In general medical drugs, valproic acid is also widely used, for example, its use in EVE Quick is very popular. EVE Quick is added with "ibuprofen" which has the ingredients of suppressing headaches, together with the ad...

Claims

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