An efficientcopper(I) iodide‐catalyzed sulfenylation of maleimides and related 3‐indolylmaleimides with thiols has been developed in the presence of fluoroboric acid. Several 3‐thiomaleimides and 3‐indolyl‐4‐thiomaleimides were obtained with good yields under ligand‐free conditions. The methods are simple, practical and show good functional group tolerance.
Reversible Covalent Linkage of Functional Molecules
申请人:Smith Mark
公开号:US20120190124A1
公开(公告)日:2012-07-26
The present invention relates to the use of a compound containing a moiety of formula (I) as a reagent for linking a compound of formula R
1
—H which comprises a first functional moiety of formula F
1
to a second functional moiety of formula F
2
wherein X, X′, Y, R
1
, F
1
and F
2
are as defined herein. The present invention also provides related processes and products. The present invention is useful for creating functional conjugate compounds, and specifically conjugates in which at least one of the constituent molecules carries a thiol group.
The present invention relates to a product comprising a solid substrate and a moiety of formula (I) linked thereto: wherein X, X′ and R are as defined herein. The product is useful for immobilising target molecules such as molecules of biochemical interest to solid substrates for numerous applications, such as affinity chromatography, ELISA, biotechnological assay techniques and solid phase peptide synthesis.
The present invention relates to the use of a compound comprising a moiety of formula (I) as a reagent for protecting a thiol group in a thiol compound
wherein X, X′ and Y are as defined herein. The protecting group methodology of the present invention allows straightforward and selective protection of thiol groups. Cleaving of the thiol group to regenerate the thiol functional group is also facile and controllable. The present invention further provides an analogous protecting group methodology directed to protection of disulfide groups.