2 with boron trifluoride etherate. With aqueous sulphuric acid the products are due to both transannular ring closure, 2, and transannular hydride migration, 3 and 4. trans-Cyclooctene derivatives 3 and 4 are formed by the trans-elimination of trimethylsilanol from the likely intermediate β-hydroxysilanes 10 and 11. The results with methanolic sulphuric acid are similar. It is also noticed that the
METHODS OF INCORPORATING AN AMINO ACID COMPRISING A BCN GROUP INTO A POLYPEPTIDE USING AN ORTHOGONAL CODON ENCODING IT AND AN ORTHORGONAL PYLRS SYNTHASE
申请人:MEDICAL RESEARCH COUNCIL
公开号:US20150148525A1
公开(公告)日:2015-05-28
The invention relates to a polypeptide comprising an amino acid having a bicyclo[6.1.0]non-4-yn-9-ylmethanol (BCN) group, particularly when said BCN group is present as: a residue of a lysine amino acid. The invention also relates to a method of producing a polypeptide comprising a BCN group, said method comprising genetically incorporating an amino acid comprising a BCN group into a polypeptide. The invention also relates to an amino acid comprising bicyclo[6.1.0]non-4-yn-9-ylmethanol (BCN), particularly and amino acid which is bicyclo[6.1.0]non-4-yn-9-ylmethanol (BCN) lysine. In addition the invention relates to a PylRS tRNA synthetase comprising the mutations Y271M, L274G and C313A.
METHODS OF INCORPORATING AN AMINO ACID COMPRISING A BCN GROUP INTO A POLYPEPTIDE USING AN ORTHOGONAL CODON ENCODING IT AND AN ORTHORGONAL PYLRS SYNTHASE.
申请人:Medical Research Council
公开号:EP2852664B1
公开(公告)日:2017-09-06
[EN] MULTIPLE CYCLOADDITION REACTIONS FOR LABELING OF MOLECULES<br/>[FR] RÉACTIONS DE CYCLOADDITION MULTIPLE POUR LE MARQUAGE DE MOLÉCULES
申请人:EUROPEAN MOLECULAR BIOLOGY LAB EMBL
公开号:WO2015107064A1
公开(公告)日:2015-07-23
The present invention relates to methods for linking tetrazines with dienophiles to establish at least two linkages by sequentially performing at least two cycloaddition reactions. The methods in particular allow establishing multi-labeling strategies. In particular, the invention relates to methods for forming linkages by cycloaddition reactions, wherein the method comprises reacting a first alkyl-substituted tetrazine with a first dienophile comprising a irans-cyclooctenyl group followed by reacting a second tetrazine with a second dienophile comprising a cyclooctynyl group, wherein the reaction of the first tetrazine with the first dienophile proceeds in the presence of the second dienophile.