Preparation method of ozanimod intermediate

The invention belongs to the technical field of drug synthesis, and provides a preparation method of an ozanimod intermediate, which comprises the following steps: by taking compound (S)-1-(2-oxooxazolidine-3-yl)-2, 3-dihydro-1H-indene-4-formonitrile as a raw material, firstly, reacting with a 50% h...

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Bibliographic Details
Main Authors ZHANG NAIHUA, BAO GUANGLONG
Format Patent
LanguageChinese
English
Published 26.04.2024
Subjects
CHEMISTRY
HETEROCYCLIC COMPOUNDS
METALLURGY
ORGANIC CHEMISTRY
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Summary:The invention belongs to the technical field of drug synthesis, and provides a preparation method of an ozanimod intermediate, which comprises the following steps: by taking compound (S)-1-(2-oxooxazolidine-3-yl)-2, 3-dihydro-1H-indene-4-formonitrile as a raw material, firstly, reacting with a 50% hydroxylamine aqueous solution and acetic acid, and then, adding a catalyst to react, thereby obtaining the ozanimod intermediate. The preparation method comprises the following steps of: adding 5-formyl-2-isopropoxy benzonitrile into a reaction kettle without separation, and then adding 5-formyl-2-isopropoxy benzonitrile to react to obtain (S)-2-isopropoxy-5-(3-(1-(2-oxooxazolidine-3-yl)-2, 3-dihydro-1H-indene-4-yl)-1, 2, 4-oxadiazole-5-yl) benzonitrile. According to the preparation method provided by the invention, the intermediate is not separated and purified, the conversion rate of reaction materials can be effectively improved, and unit operation is simplified. The side reaction caused by the selection of acid
Bibliography:Application Number: CN202211263200