A solid-phase technology for the preparation of amides

C - Chemistry – Metallurgy – 07 – C

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C07C 231/10 (2006.01) C07C 47/565 (2006.01) C07C 51/367 (2006.01) C07C 59/125 (2006.01) C07C 59/74 (2006.01) C07C 69/708 (2006.01) C07C 69/712 (2006.01) C07K 1/00 (2006.01) C07K 1/04 (2006.01)

Patent

CA 2269589

A method for the solid phase synthesis of compounds of formula (1), in which either or both of R1 or R2 are combinatorially variable by a process represented by scheme (4) and wherein: X is (a), (b), (c) or (d); Y is H or a side chain functional group protective moiety such as Fmoc; R2' is an intermediate form of R2 which is subsequently chemically transformed to give the desired R2; and n is between 2 and 12, preferably 4. The invention also provides compounds and combinatorial libraries of compounds of formula (1), as well as intermediate compounds for use in the method.

L'invention concerne un procédé permettant la synthèse en phase solide de composés de la formule (1), dans laquelle R<1> et/ou R<2> sont variables, de manière combinatoire, suivant un procédé représenté par le schéma (4) où X represente (a), (b), (c) ou (d) où Y représente H ou une fraction protectrice de groupe fonctionnel à chaîne latérale, tel que Fmoc, où R2<1> représente une forme intermédiaire de R2 qu'on transforme ensuite chimiquement en vue d'obtenir le R2 voulu, et où n est compris entre 2 et 12, et est égal, de préférence, à 4. L'invention concerne également des composés et des banques combinatoires de composés de la formule 1, ainsi que des composés intermédiaires destinés à l'utilisation dans ledit procédé.

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