Proton acceptor iminium/carbocation-type coupling agents
AssigneeLuxembourg Bio Technologies Ltd.
InventorsFernando Albericio, Ayman El-Faham, Yoav Luxembourg, Ariel Ewenson
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Abstract
Novel iminium-type coupling agents containing proton acceptors in their iminium moiety, which can be used beneficially as coupling agents in various chemical polypeptide and/or polynucleotide syntheses, and are particularly useful as yield enhancing and racemization suppressing coupling agents for use in peptide syntheses, are disclosed. Further disclosed are a process of preparing such iminium-type coupling agents and their use in the preparation of polypeptides and/or polynucleotides.
Claims39
1-42. (canceled)
A coupling agent having a general formula selected from the group consisting of:
- wherein:
- A is an inorganic anion;
- L is a leaving group;
- n is an integer from 1 to 4,
- each of R1, R2, R3, R4, R5 and R6 is independently selected from the group consisting of an alkyl having 1-4 carbon atoms and an alkyl having 1-4 carbon atoms interrupted, substituted and/or terminated by at least one heteroatom, or, alternatively, R1 and R2, and/or R3 and R4, and/or R5 and R6 are each independently joined to form a heteroalicyclic moiety,
- provided that:
- at least one of R1, R2, R3, R4, R5 and R6 is an alkyl having 1-4 carbon atoms interrupted, substituted and/or terminated by at least one heteroatom and/or at least one of R1 and R2, and/or R3 and R4, and/or R5 and R6 are joined to form a heteroalicyclic moiety.
A coupling agent selected from the group consisting of:
A coupling agent being
Dependencies are inferred from the claim text.