Patent ID: 6756492
Filing Date: 2004-06-29
Classification: B01J,B82Y,C07B,C07H,C40B,Y02P

Abstract:
Nucleoside derivatives having photolabile protective group of general formula (I). in whichR1=H, NO2, CN, OCH3, halogen, an alkyl, alkoxy or alkoxyalkyl residue having 1 to 4 C atoms or an optionally substituted aryl residue or an aliphatic acyl residue having 2 to 5 atoms, R2=H, NO2, CN, OCH3, halogen, an alkyl, alkoxy or alkoxyalkyl residue having 1 to 4 C atoms or an optionally substituted aryl residue or an aliphatic acyl residue 2 to 5 atoms, R3=H, halogen, NO2, CN, OCH3, an alkyl, alkoxy or alkoxyalkyl residue having 1 to 4 C atoms or an optionally substituted aryl residue or aliphatic acyl residue having 2 to 5 C atoms, R4=H, halogen, NO2, CN, OCH3, an alkyl, alkoxy, or alkoxyalkyl residue having 1 to 4 C atoms or an optionally substituted aryl residue or aliphatic acyl residue having 2 to 5 atoms, R5=H, dimethoxytrityl or a protective group common in the chemistry of nucleotides or a functional group common for the production of oligonucleotides, R6=H, OH, halogen or &PSgr;R8, wherein &PSgr;=O or S and R8=alkyl or alkoxyalkyl having 1 to 4 C atoms or an optionally substituted aryl residue or an aliphatic acyl residue having 2 to 5 atoms and a protective group common in the chemistry of nucleotides, R7=H, NO2, CN, OCH3, halogen, an alkyl, alkoxy or alkoxyalkyl residue having 1 to 4 C atoms or an optionally substituted aryl residue or aliphatic acyl residue having 2 to 5 atoms, n=0 or 1, X=SO2, OC(O), OC(S) with the proviso that in case X=Oâ€”C(O) nâ‰ 0, B=H, adenine, cytosine, guanine, thymine, uracil, 2,6-diaminopurine-9-yl, hypoxanthine-9-yl, 5-methylcytosine-1-yl, 5-amino-4imidazole carboxylic acid-1-yl or 5-amino-4-imadazole carboxylic acid amide-3-yl, wherein in case B=adenine, cytosine or guanine the primary amino function optionally has a temporary or permanent protective group and/or thymine or uracil optionally has a permanent protective group at the O4 position.