2,N.sup.6 -disubstituted and 2,N.sup.6 -trisubstituted adenosine-3'-phosphoramidites
First Claim
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1. Adenosines having the formula:
- ##STR15## in which one of --OR7 and --OR8 is a phosphite or a phosphoramidite group of the formula ##STR16## and the other of --OR7 and --OR8 or --OR4, and wherein;
R1 is a lower alkyl radical or --(CH2)n --CN, n being an integer of from 1 to 4;
X is a halogen atom, an amino group, or a member selected from the group consisting of tetrazolyl, imidazolyl, nitroimidazolyl, indolyl, pyrazolyl, benzimidazolyl, isoindolyl, pyrrolyl, triazolyl, dioxazolyl, dialkylamino, morpholino, pyrrolidino and piperidino groups;
R4 is a hydroxyl protecting group;
R2 is --NH(A1) or --N(A1, A2);
R3 is --NH(A1), --N(A1, A2), --O(A1) or --S(A1);
A1 and A2 are identical or different and are selected from the group consisting of hydrogen and acyl groups;
R5 is a hydrogen atom or a group --OR6, wherein R6 is hydrogen, an acyl group or a hydroxyl protecting group.
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Abstract
The invention concerns 2,N6 -disubstituted and 2,N6 -trisubstituted adenosine nucleosides in which the sugar component is substituted at position 3'"'"' or position 5'"'"' by a phosphite or phosphoramidite group of the formula: ##STR1## R1 representing a lower alkyl or --(CH2)n --CN with n being an integer between 1 and 4, and X representing a halogen or an amine group. These nucleosides make it possible to prepare sequences of nucleotides usable, in particular, as probes in the field of analyses and biological extractions.
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Citations
6 Claims
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1. Adenosines having the formula:
- ##STR15## in which one of --OR7 and --OR8 is a phosphite or a phosphoramidite group of the formula ##STR16## and the other of --OR7 and --OR8 or --OR4, and wherein;
R1 is a lower alkyl radical or --(CH2)n --CN, n being an integer of from 1 to 4;X is a halogen atom, an amino group, or a member selected from the group consisting of tetrazolyl, imidazolyl, nitroimidazolyl, indolyl, pyrazolyl, benzimidazolyl, isoindolyl, pyrrolyl, triazolyl, dioxazolyl, dialkylamino, morpholino, pyrrolidino and piperidino groups; R4 is a hydroxyl protecting group; R2 is --NH(A1) or --N(A1, A2); R3 is --NH(A1), --N(A1, A2), --O(A1) or --S(A1); A1 and A2 are identical or different and are selected from the group consisting of hydrogen and acyl groups; R5 is a hydrogen atom or a group --OR6, wherein R6 is hydrogen, an acyl group or a hydroxyl protecting group. - View Dependent Claims (2, 3, 4, 5, 6)
- ##STR15## in which one of --OR7 and --OR8 is a phosphite or a phosphoramidite group of the formula ##STR16## and the other of --OR7 and --OR8 or --OR4, and wherein;
Specification