Difluoromethylation reaction of paracarbonyl copound participated with [(phenylsulfonyl) difluoromethyl] trimethyl silane

A technology of carbonyl compounds and trimethylsilane, which is applied in the field of high-efficiency difluoromethylation reagent-[difluoromethyl]trimethylsilane, which can solve the problems of reduced utilization, excessive carbonyl substrates, non-compliance with environmental protection, etc. problems, to achieve the effect of easy condition control and high yield
CN1295202CInactive Publication Date: 2007-01-17SHANGHAI INST OF ORGANIC CHEM CHINESE ACAD OF SCI
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
SHANGHAI INST OF ORGANIC CHEM CHINESE ACAD OF SCI
Publication Date
2007-01-17
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention relates to a process for synthesizing difluoro methanol product yield including difluoro methanol from difluoro-methylation reaction of ((phenylsulfonyl) difluoromethyl) trimethyl silicane adding carbonyl compound (aldehyde or ketone), the process consists of fluorinion-initiated (phenylsulfonyl) difluoromethyl methylation reaction and magnesium-participated reduction de-sulfonation reaction, The advantages of the disclosed process include simple process, high yield, economy and reaction environment friendliness.
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Description

technical field

[0001] The invention relates to a high-efficiency difluoromethylation reagent-[(benzenesulfonyl)difluoromethyl]trimethylsilane (TMSCF 2 SO 2 Ph), used this reagent for the first time to achieve the difluoromethylation reaction of catalytic carbonyl compounds under the trigger of fluoride ion. TMSCF 2 SO 2 Ph reagent is an important difluoromethylation reagent for the synthesis of fluorine-containing drugs and fluorine-containing materials. The method of the invention is a difluoromethylation reaction initiated by fluoride ions and a selective desulfone reaction participated in by metal magnesium, and is an environment-friendly reaction. Background technique

[0002] Fluorochemicals are widely used in drug design and new material development. The selective introduction of fluorine atoms or fluorine-containing building blocks into organic molecules can greatly enhance the biological activity of these molecules. Therefore, the research on selective fluorin...

Claims

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