Ribonucleic acid compound and method of liquid-phase...

C - Chemistry – Metallurgy – 07 – H

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C07H 19/10 (2006.01) A61K 31/7068 (2006.01) A61K 31/7072 (2006.01) A61K 31/7076 (2006.01) A61K 31/7088 (2006.01) C07H 19/20 (2006.01) C07H 21/02 (2006.01) C07H 21/04 (2006.01)

Patent

CA 2554618

A novel ribonucleic acid compound in a phosphoric triester form. It is important for the liquid-phase synthesis of an oligo RNA. It is a ribonucleic acid compound represented by the following general formula. In the formula, B represents adenine, guanine, cytosine, uracil, or a modification of any of these; R21 represents optionally substituted aryl or optionally substituted, mono- or bicyclic, heterocyclic group; R20 represents hydrogen or optionally substituted alkyl; and R1 represents a protective group at least 90% of which can be eliminated in 24 hours at any temperature in the range of 0 to 60~C under acid conditions of a pH of 2 to 4.

Cette invention se rapporte à un nouveau composé d'acide ribonucléique sous la forme de triester phosphorique. Ce composé est important pour la synthèse en phase liquide d'un acide oligo-ribonucléique. Ce composé d'acide ribonucléique est représenté par la formule générale (I). Dans cette formule, B représente adénine, guanine, cytosine, uracil ou une modification de ceux-ci ; R?21¿ représente aryle éventuellement substitué ou un groupe hétérocyclique, monocyclique ou bicyclique, éventuellement substitué ; R?20¿ représente hydrogène ou alkyle éventuellement substitué ; et R?1¿ représente un groupe protecteur dont au moins 90 % peut être éliminé en 24 heures à une température comprise entre 0 et 60 ·C dans des conditions acides avec un pH compris entre 2 et 4.

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