A bifunctional linker of Formula 1

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wherein in Formula I, at least one of R.sup.1 to R.sup.4 is —COOR.sup.5 and R.sup.5 is —C.sub.0-C.sub.10alkyl(C.sub.2-C.sub.10alkynyl) or —C.sub.0-C.sub.10alkyl-C.sub.2-C.sub.10alkenyl(C.sub.2-C.sub.10alkynyl), preferably a terminal alkynyl. The bifunctional linker is used in a cycloaddition to tether two entities, for example a protein or antibody, and an active agent, to form a bisconjugate. The bifunctional linker also be used to form a conjugate, followed by cycloaddition in the presence of a comonomer composition to form a bisconjugate including a protein or antibody linked to an adhesive polymer network. Catalysis can be provided by a copper-containing paint on a surface to adhere the bisconjugate to the surface. Methods of synthesis and use of the bisconjugates imaging, diagnostic, and therapeutic applications are also described.

A bifunctional linker of Formula 1

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wherein in Formula I, at least one of R.sup.1 to R.sup.4 is —COOR.sup.5 and R.sup.5 is —C.sub.0-C.sub.10alkyl(C.sub.2-C.sub.10alkynyl) or —C.sub.0-C.sub.10alkyl-C.sub.2-C.sub.10alkenyl(C.sub.2-C.sub.10alkynyl), preferably a terminal alkynyl. The bifunctional linker is used in a cycloaddition to tether two entities, for example a protein or antibody, and an active agent, to form a bisconjugate. The bifunctional linker also be used to form a conjugate, followed by cycloaddition in the presence of a comonomer composition to form a bisconjugate including a protein or antibody linked to an adhesive polymer network. Catalysis can be provided by a copper-containing paint on a surface to adhere the bisconjugate to the surface. Methods of synthesis and use of the bisconjugates imaging, diagnostic, and therapeutic applications are also described.

Provided is a method for producing a chlorophenoxycarboxylate, comprising the following steps of: a phenoxycarboxylate under actions of a catalyst A and a catalyst B performing a selective chlorination of a chlorinating agent at a 2-position and/or a 4-position to obtain the chlorophenoxycarboxylate; the catalyst A is a Lewis acid; and the catalyst B has the following structure: R.sub.1′—S—R.sub.2′. The present disclosure redesigns the process route, and finely screens the catalyst and the chlorinating agent, thereby effectively improving the chlorination selectivity while avoiding the loss of the active ingredient, and the content of the obtained chlorophenoxycarboxylate can reach more than 98.5%, and the yield can reach more than 99%.

Provided is a method for producing a chlorophenoxycarboxylate, comprising the following steps of: a phenoxycarboxylate under actions of a catalyst A and a catalyst B performing a selective chlorination of a chlorinating agent at a 2-position and/or a 4-position to obtain the chlorophenoxycarboxylate; the catalyst A is a Lewis acid; and the catalyst B has the following structure: R.sub.1′—S—R.sub.2′. The present disclosure redesigns the process route, and finely screens the catalyst and the chlorinating agent, thereby effectively improving the chlorination selectivity while avoiding the loss of the active ingredient, and the content of the obtained chlorophenoxycarboxylate can reach more than 98.5%, and the yield can reach more than 99%.

Disclosed is a method for preparing a benzofuran derivative. In particular, provided is a method for preparing a benzofuran derivative, wherein according to the method provided, reaction steps required to synthesize the benzofuran substance in the prior art can be effectively shortened.

Disclosed is a method for preparing a benzofuran derivative. In particular, provided is a method for preparing a benzofuran derivative, wherein according to the method provided, reaction steps required to synthesize the benzofuran substance in the prior art can be effectively shortened.

Disclosed is a method for preparing a benzofuran derivative. In particular, provided is a method for preparing a benzofuran derivative, wherein according to the method provided, reaction steps required to synthesize the benzofuran substance in the prior art can be effectively shortened.

The invention includes procedures for stereoselective β-acylation of carboxylic acids having a β-carbon atom. For example, stereoselective acylation procedures include the following reactions: (I) ##STR00001##

The invention includes procedures for stereoselective β-acylation of carboxylic acids having a β-carbon atom. For example, stereoselective acylation procedures include the following reactions: (I) ##STR00001##

The invention includes procedures for stereoselective -acylation of carboxylic acids having a -carbon atom. For example, stereoselective acylation procedures include the following reactions: (I)

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