C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 307/79 (2006.01) C07K 1/04 (2006.01) C07K 1/06 (2006.01)
Patent
CA 2662653
The present invention is directed to a method for .alpha.N-methylation of amino acids suitable for on-resin methylation, compatible with Fmoc/tBu SPPS, and compatible with amino acids bearing protected or unprotected nucleophilic side-chains, notably Arg(Pbf), Met, Cys, and Trp. The present invention is further directed to a compound of Formula I (see formula I) wherein m, n, X and Y are defined as described herein.
La présente invention concerne une méthode d'alpha-N-méthylation des acides aminés convenant pour la méthylation sur résine, compatible avec SPPS sur Fmoc/tBu, et compatible avec les acides aminés portant des chaînes latérales nucléophiles protégées ou non, entre autres Arg(Pbf), Met, Cys et Trp. La présente invention a également trait à un composé de formule I (voir la formule I), où m, n, X et Y sont tels que définis ici.
Moss Jason A.
Swistok Joseph
F. Hoffmann-La Roche Ag
Gowling Lafleur Henderson Llp
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