N.alpha.-2-(4-nitrophenylsulfonyl)ethoxycarbonyl-amino acids

Details N.alpha.-2-(4-nitrophenylsulfonyl)ethoxycarbonyl-amino acids N.alpha.-2-(4-nitrophenylsulfonyl)ethoxycarbonyl-amino acids

C - Chemistry, Metallurgy

07

C

C07C 323/59 (2006.01) C07C 317/18 (2006.01) C07C 317/48 (2006.01) C07D 207/16 (2006.01) C07D 209/20 (2006.01) C07D 233/64 (2006.01) C07D 311/84 (2006.01) C07D 473/06 (2006.01) C07K 1/06 (2006.01)

Patent

CA 2212052

Protected amino acid derivatives of general formula (I) wherein R1 represents hydrogen atom, and R2 represents hydrogen, methyl, isopropyl, 1-methylpropyl, 2-methylpropyl, tert-butoxymethyl, 1-tert-butoxyethyl, 2-methylthioethyl, benzyl, carboxamidomethyl, 2-carboxamidoethyl, tert-butoxycarbonylmethyl, 2- (tert-butoxycarbonyl)ethyl, 4-(tert-butoxycarbamido)butyl, 4-tert- butoxybenzyl, indolyl-3-methyl, S(triphenylmethyl)thiomethyl, 1- (triphenylmethyl)imidazolyl-4-methyl, 3-(NG- mesitylenesulfonyl)guanidinopropyl, N-xanthylcarboxamidomethyl, 2-(N- xanthylcarboxamido)ethyl or S-(acetamidomethyl)thiomethyl; or R1 and R2 together represent propylene radical. Methods for the preparation of said derivatives are provided, and a process for solid phase peptide synthesis using said derivatives is described.

Dérivés d'acides aminés protégés répondant à la formule générale (I), dans laquelle R¿1? représente un atome d'hydrogène, et R¿2? représente hydrogène, méthyle, isopropyle, 1-méthylpropyle, 2-méthylpropyle, tert-butoxyméthyle, 1-tert- butoxyéthyle, 2-méthylthioéthyle, benzyle, carboxamidométhyle, 2-carboxamidoéthyle, tert-butoxycarbonylméthyle, 2-(tert-butoxycarbonyl)éthyle, 4-(tert-butoxycarbamido)butyle, 4-tert-butoxybenzyle, indolyl-3-méthyle, S-(triphénylméthyl)thiométhyle, 1-(triphénylméthyl)imidazolyl-4-méthyle, 3-(N?G¿-mésitylènesulfonyl)guanidinopropyle, N-xanthylcarboxamidométhyle, 2-(N-xanthylcarboxamido)éthyle ou S-(acétamidométhyl)thiométhyle; ou R¿1? et R¿2?, pris ensemble, représentent un radical propylène. On a également prévu des procédés de préparation de ces dérivés, ainsi qu'un procédé de synthèse de peptides en phase solide mettant en oeuvre lesdits dérivés.

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