Catalyst composition and use of catalyst composition or catalyst for catalyzing nucleophilic substitution reactions

Abstract

The present invention provides a catalyst composition comprising: (a) at least one catalyst, (b) at least one silicon additive, and (c) optionally a base. The present invention also provides the catalyst composition or catalyst according to the present invention for catalyzing 2 Use of a nucleophilic substitution reaction of a compound of the F group with a nucleophile. Catalyst or catalyst composition according to the present invention can fully activate the 2 F group compounds and nucleophiles, so that they can efficiently carry out nucleophilic substitution reactions. In addition, the nucleophilic substitution reaction using the catalyst composition or catalyst according to the present invention is easy to operate, has high yield, and is suitable for large-scale production.

Description

technical field [0001] The invention relates to the field of organic synthesis, in particular to a catalyst composition and the use of the catalyst composition or catalyst for catalyzing nucleophilic substitution reactions. Background technique [0002] Due to its stable chemical properties and good functional group compatibility, sulfonyl fluoride plays a very important role in synthetic chemistry, and has increasingly attracted the attention of chemists and pharmacologists. Compared with sulfonyl chloride, the reaction between sulfonyl fluoride and nucleophile has disadvantages such as low efficiency and narrow substrate range. The development of a catalyst system for activating the nucleophilic substitution reaction of sulfonyl fluoride is an important and difficult point in the field of sulfonyl fluoride research. [0003] The methods reported in the literature to activate the nucleophilic substitution reaction of sulfonyl fluoride are very limited. For example, CN 107...

AI Technical Summary

Problems solved by technology

This system requires the use of a large amount of expensive Ca(NTf 2 ) 2 , which increases the production cost, severely limits the large-scale application of this method in synthesis, and also brings inconvenience to separation and purification; at the same time, this method also lacks reports on substrates with large steric hindrance

[0005] As mentioned above, containing -SO 2 The activation of compounds of the F group has the following problems: 1) there is no broad-spectrum mild method; 2) it is necessary to use stoichiometric expensive metal salts such as Ca(NTf 2 ) 2 , is not suitable for industrial scale use and does not meet the requirements of green chemistry; 3) in the presence of -SO 2 In the reaction of F group compounds with nucleophiles, the reactivity depends heavily on the -SO 2 The chemical properties of the compound of the F group and the nucleophile, the scope of the substrate is limited

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