The synthetic method of 4-methanesulfonylbutyl isothiocyanate

Abstract

The invention relates to a chemical synthesis method of 4-methanesulfonylbutyl isothiocyanate (Erysolin). The method comprises that 1-bromo-4-chlorobutane and hydrous sodium methyl mercaptide as starting raw materials undergo a reaction to produce chlorothioether, the chlorothioether and phthalimide potassium salt undergo a reaction to produce a tertiary amine conjugate, the tertiary amine conjugate undergoes a hydrazinolysis reaction to produce thioether primary amine, the thioether primary amine forms isothiocyanate under action of thiophosgene, and the isothiocyanate is oxidized to form Erysolin. The chemical synthesis method is simple in operation, uses a small amount of dangerous reagents, gives consideration to a cost and a yield and is suitable for Erysolin industrial production.

Description

technical field

[0001] The present invention relates to a kind of chemical synthesis method of 4-methanesulfonyl butyl isothiocyanate (Erysolin), especially relate to a kind of 4-butane with 1-bromo-4-chlorobutane, aqueous sodium methyl mercaptide as initial raw material Synthetic method of methanesulfonyl butyl isothiocyanate. Background technique

[0002] Erysolin, also known as 4-methylsulfonyl butyl isothiocyanate, is named because it comes from the genus Erysimum of the Brassicaceae. Its molecular formula is C 6 h 11 NO 2 S 2 , the relative molecular mass is 193.29, white to light lemon-colored crystals, and its structural formula is as follows:

[0003]

[0004] Studies have found that isothiocyanate has good anti-tumor and anti-nerve damage effects, and this type of compound is mainly derived from the cruciferous plant Saccharomyces genus. ERY plays a unique role in anti-tumor, especially for tumor cells with multi-drug resistance to chemotherapy drugs and P5...

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