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1. (WO1999009041) SOLUTION PHASE SYNTHESIS OF OLIGONUCLEOTIDES
Latest bibliographic data on file with the International Bureau   

Pub. No.: WO/1999/009041 International Application No.: PCT/GB1998/002407
Publication Date: 25.02.1999 International Filing Date: 10.08.1998
Chapter 2 Demand Filed: 17.02.1999
IPC:
C07D 207/48 (2006.01) ,C07D 265/33 (2006.01) ,C07F 9/165 (2006.01) ,C07F 9/18 (2006.01) ,C07H 19/10 (2006.01) ,C07H 19/20 (2006.01) ,C07H 21/00 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
207
Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
46
with hetero atoms directly attached to the ring nitrogen atom
48
Sulfur atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
265
Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
28
1,4-Oxazines; Hydrogenated 1,4-oxazines
30
not condensed with other rings
32
with oxygen atoms directly attached to ring carbon atoms
33
Two oxygen atoms, in positions 3 and 5
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
F
ACYCLIC, CARBOCYCLIC, OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
9
Compounds containing elements of the 5th Group of the Periodic System
02
Phosphorus compounds
06
without P-C bonds
16
Esters of thiophosphoric acids or thiophosphorous acids
165
Esters of thiophosphoric acids
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
F
ACYCLIC, CARBOCYCLIC, OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
9
Compounds containing elements of the 5th Group of the Periodic System
02
Phosphorus compounds
06
without P-C bonds
16
Esters of thiophosphoric acids or thiophosphorous acids
165
Esters of thiophosphoric acids
18
with hydroxyaryl compounds
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
H
SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
19
Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro derivatives thereof
02
sharing nitrogen
04
Heterocyclic radicals containing only nitrogen as ring hetero atom
06
Pyrimidine radicals
10
with the saccharide radical being esterified by phosphoric or polyphosphoric acids
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
H
SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
19
Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro derivatives thereof
02
sharing nitrogen
04
Heterocyclic radicals containing only nitrogen as ring hetero atom
16
Purine radicals
20
with the saccharide radical being esterified by phosphoric or polyphosphoric acids
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
H
SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
21
Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids
Applicants:
REESE, Colin, Bernard [GB/GB]; GB (UsOnly)
SONG, Quanlai [CN/US]; US (UsOnly)
AVECIA LIMITED [GB/GB]; Hexagon House Blackley, P.O. Box 42 Manchester M9 8ZS, GB (AL, AM, AT, AU, AZ, BA, BB, BE, BF, BG, BJ, BR, BY, CA, CF, CG, CH, CI, CM, CN, CU, CY, CZ, DE, DK, EE, ES, FI, FR, GA, GB, GE, GH, GM, GN, GR, GW, HR, HU, ID, IE, IL, IS, IT, JP, KE, KG, KP, KR, KZ, LC, LK, LR, LS, LT, LU, LV, MC, MD, MG, MK, ML, MN, MR, MW, MX, NE, NL, NO, NZ, PL, PT, RO, RU, SD, SE, SG, SI, SK, SL, SN, SZ, TD, TG, TJ, TM, TR, TT, UA, UG, UZ, VN, YU, ZW)
Inventors:
REESE, Colin, Bernard; GB
SONG, Quanlai; US
Agent:
REVELL, Christopher; Avecia Limited Intellectual Porperty Group P.O. Box 42, Hexagon House Blackley Manchester M9 8ZS , GB
Priority Data:
9717158.113.08.1997GB
Title (EN) SOLUTION PHASE SYNTHESIS OF OLIGONUCLEOTIDES
(FR) SYNTHESE EN PHASE DE SOLUTION D'OLIGONUCLEOTIDES
Abstract:
(EN) A process for the synthesis in solution phase of a phosphorothioate triester is provided. The process comprises the solution phase coupling of an H-phosphonate with an alcohol in the presence of a coupling agent to form an H-phosphonate diester. The H-phosphonate diester is oxidised in situ with a sulfur transfer agent to produce the phosphorothioate triester. Preferably, the H-phosphonate and alcohol are protected nucleosides or oligonucleotides. Oligonucleotide H-phosphonates which can be used in the formation of phosphorothioate triesters are also provided.
(FR) Procédé servant à effectuer la synthèse dans une phase de solution d'un triester de phosphorothioate. Ce procédé consiste à coupler la phase de solution d'un H-phosphonate avec un alcool en présence d'un agent de couplage afin d'obtenir un diester de H-phosphonate. On oxyde ce diester de H-phosphonate in situ par un agent de transfert de soufre, de manière à obtenir le triester de phosphorothioate. Le H-phosphonate et l'alcool sont, de préférence, des nucléosides ou des oligonucléotides protégés. L'invention concerne également des H-phosphonates d'oligonucléotides qu'on peut utiliser afin de produire des triesters de phosphorothioate.
Designated States: AL, AM, AT, AU, AZ, BA, BB, BG, BR, BY, CA, CH, CN, CU, CZ, DE, DK, EE, ES, FI, GB, GE, GH, GM, HR, HU, ID, IL, IS, JP, KE, KG, KP, KR, KZ, LC, LK, LR, LS, LT, LU, LV, MD, MG, MK, MN, MW, MX, NO, NZ, PL, PT, RO, RU, SD, SE, SG, SI, SK, SL, TJ, TM, TR, TT, UA, UG, US, UZ, VN, YU, ZW
African Regional Intellectual Property Organization (ARIPO) (GH, GM, KE, LS, MW, SD, SZ, UG, ZW)
Eurasian Patent Office (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (EPO) (AT, BE, CH, CY, DE, DK, ES, FI, FR, GB, GR, IE, IT, LU, MC, NL, PT, SE)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GW, ML, MR, NE, SN, TD, TG)
Publication Language: English (EN)
Filing Language: English (EN)