Synthesis method of etretinate ether

A compound, selected technology, applied in the preparation of carboxylate, chemical instruments and methods, preparation of organic compounds, etc., can solve the problems of unsafe operation, harsh reaction conditions, long reaction time, etc. mild effects
CN101747194BActive Publication Date: 2013-05-01CHONGQING HUAPONT PHARMA

Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
CHONGQING HUAPONT PHARMA
Publication Date
2013-05-01

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Abstract

The invention relates to a synthesis method of etretinate ether. The synthesis method adopts (1-(5, 6, 7, 8-tetrahydrophthalic-5, 5, 8, 8-tetramethyl-2-naphthyl)-ethyl)-terphenyl phosphorus halide (II) and p-eormylbenzoic acid ester (III) as raw materials, carries out two-phase reaction under the condition of adding aqueous alkali into an organic solvent, and then obtains the etretinate ether. The method has mild reaction condition, short reaction time, simple and convenient operation, low cost and high yield.
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Description

technical field

[0001] The present invention relates to the synthesis method of aromatic retinoic acid ester. Background technique

[0002] Aromatic retinoids have high medicinal value. U.S. Patent No. 4,326,055 discloses [1-(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthyl)-ethyl]-triphenylphosphine halide and p-ethoxy Carbocarbonylbenzaldehyde was subjected to Wittig reaction, under the protection of inert gas, reacted for 12 hours at 65°C to obtain p-[(E)-2-(5,6,7,8-tetrahydro-5,5,8,8- Tetramethyl 1-2-naphthyl) propenyl]-ethyl benzoate; CN200510020500.2 discloses the preparation method of aromatic ethyl retinoic acid ester, [1-(5,6,7,8-tetrahydro-5 , 5,8,8-tetramethyl-2-naphthyl)-ethyl]-triphenylphosphine bromide, p-ethoxycarbonylbenzaldehyde, add isopropanol, blow nitrogen, when heated to 65°C, add Ethanol and sodium metal were reacted for 11 hours, and the solvent was removed. Methanol was added to the residue, and the solid was separated to obtain the crude product...

Claims

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