C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 209/48 (2006.01) C07H 21/00 (2006.01) C07K 1/04 (2006.01) C40B 50/14 (2006.01)
Patent
CA 2647260
A compound which can be attached to a solid support and used as a reagent for methods of solid phase synthesis has the following structure: (I) where Ri is selected from hydrogen and C1-C6 alkyl; R2 is selected from hydrogen, hydroxy, and C1-C6 alkoxy, or together R1and R2 form a single bond; R3, R4, R5 and R6 are the same or different from each other and each represents hydrogen, C1-C6 alkyl, and halogen, or together R3 and R4 with R5 and R6 form an aromatic ring, further wherein the aromatic ring is substituted with one or more X; X is selected from halogen, nitro, amino, and aminocarbonyl; s is 0, 1, 2, or 3, t is 0, 1, 2, or 3, wherein s + t >=1; R7 and R8 are the same or different from each other and each represents hydroxy, halogen, hydrogen, C1-C6 alkoxy, oxyacyl, or together R7 and R8 form a carbonyl; Y is selected from a methylene or substituted methylene, nucleoside, nucleotide, protected nucleoside, protected nucleotide, C1-C6 aryl, arylalkyl, heteroalkyl, heterocycle, and heteroaryl; n is 1, 2, 3, 4, 5, 6, 7, 8, 9, or 10; Z is selected from OR and NHR; R is selected from hydrogen, SiRa,RbRc, CRaRb, Rc, heteroalkyl, and C1-C6 alkyl; Ra, Rb, and Rc are the same as or different from each other and each represents methyl, ethyl, i-propyl, t-butyl, phenyl or substituted phenyl.
La présente invention concerne un composé pouvant se lier à un support solide et utilisé comme réactif pour des procédés de synthèse en phase solide de formule (I), dans laquelle: R1 est choisi parmi l'hydrogène, et alkyle C1-C6; R2est choisi parmi l'hydrogène, hydroxy, et alcoxy C1-C6, ou R1 et R2 ensemble forment une liaison simple; R3, R4, R5 et R6, identiques ou différents, représentent chacun l'hydrogène, alkyle C1-C6, et halogène, ou R3 et R4 ensemble avec R5 et R6 forment un noyau aromatique, ledit noyau aromatique étant en outre substitué avec un ou des X; X est choisi parmi halogène, nitro, amino, et aminocarbonyle; s est 0, 1, 2, ou 3; t est 0, 1, 2, ou 3, où s + t >= 1; R7 et R8, identiques ou différents, représentent chacun hydroxy, halogène, hydrogène, alcoxy C1-C6, oxyacyle, ou R7 et R8 ensemble forment un carbonyle; Y est choisi parmi méthylène ou méthylène substitué, nucléoside, nucléotide, nucléoside protégé, nucléotide protégé, aryle C5-C8, aralalkyle, hétéroalkyle, hétérocycle, et hétéroaryle; n est 1, 2, 3, 4, 5, 6, 7, 8, 9, ou 10; Z est choisi parmi OR et NHR. R est choisi parmi hydrogène, SiRa,RbRc, CRaRb, Rc, hétéroalkyle, Ra, Rb, et Rc, identiques ou différents, représentent chacun méthyle, éthyle, i-propyle, t-butyle, phényle ou phényle substitué.
Hatala Paul J.
Kurz Markus
Archemix Corp.
Hatala Paul J.
Kurz Markus
Ridout & Maybee Llp
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