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1. (WO1998049181) NOVEL SULFUR TRANSFER REAGENTS FOR OLIGONUCLEOTIDE SYNTHESIS
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/1998/049181 International Application No.: PCT/US1998/008763
Publication Date: 05.11.1998 International Filing Date: 30.04.1998
Chapter 2 Demand Filed: 30.11.1998
IPC:
C07F 9/165 (2006.01) ,C07H 21/00 (2006.01)
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
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:
HYBRIDON, INC. [US/US]; 155 Fortune Boulevard Milford, MA 01757, US
Inventors:
TANG, Jin, Yan; US
ZHANG, Zhaoda; US
NICHOLS, Alexandra; US
Agent:
KEOWN, Wayne, A. ; Hale and Dorr LLP 60 State Street Boston, MA 01209, US
Priority Data:
08/846,42730.04.1997US
Title (EN) NOVEL SULFUR TRANSFER REAGENTS FOR OLIGONUCLEOTIDE SYNTHESIS
(FR) NOUVEAUX REACTIFS DE TRANSFERT DE SOUFRE POUR LA SYNTHESE D'OLIGONUCLEOTIDES
Abstract:
(EN) The invention relates to the chemical synthesis of oligonucleotides and to chemical entities useful in such synthesis. More particularly, the invention relates to sulfurization of the internucleoside linkages of oligonucleotides. The invention provides new sulfur transfer reagents of formula (1) and processes for their use in sulfurizing oligonucleotides. The sulfur transfer reagents according to the invention are inexpensive to make, stable in storage, and highly efficient in sulfurization. In Formula (1) n = 1 to 4, and wherein R can be the same as or different from R1, and wherein R and R1 are selected from the group consisting of CH3, CH2CH3, tert-butyl, Formula (2), (3), (4), wherein R2, R3 and R4, are selected from the group consisting of Cl, Br, I, CN, NO2, CH3, and CH2CH3, and wherein R1, R2, R3 and R4, taken separately are hydrogen, lower alkyl, electron-withdrawing substituted lower alkyl, lower alkyl- or halo-substituted aryl, or a heterocycle containing nitrogen, oxygen, or sulfur and from 5-8 carbon atoms.
(FR) Synthèse chimique d'oligonucléotides et entités chimiques utiles pour ladite synthèse. Plus particulièrement, la présente invention concerne la sulfurisation des liaisons internucléosidiques d'oligonucléotides. Elle concerne encore de nouveaux réactifs de transfert de soufre de formule (1) et des procédés d'utilisation desdits réactifs pour la sulfurisation des oligonucléotides. Dans la formule (1), n est 1 à 4, R peut être identique à R1 ou différent de lui, R et R1 sont choisis dans le groupe constitué de CH3, CH2CH3, tert-butyle et de substances de formule (2), (3), et (4) dans lesquelles R2, R3 et R4 sont choisis dans le groupe constitué de Cl, Br, I, CN, NO2, CH3 et CH2CH3. R1, R2, R3 et R4 pris séparément sont hydrogène, alkyle inférieur, alkyle inférieur substitué à attraction d'électrons, aryle à substitution alkyle inférieur ou halo, ou un hétérocycle contenant azote, oxygène ou soufre et de 5 à 8 atomes de carbone. Les réactifs selon la présente invention sont peu onéreux pour ce qui est de leur fabrication, stables au stockage et provoquent une sulfurisation très efficace.
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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, HU, 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, UZ, VN, YU, ZW
African Regional Intellectual Property Organization (ARIPO) (GH, GM, KE, LS, MW, SD, SZ, UG, ZW)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (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, ML, MR, NE, SN, TD, TG)
Publication Language: English (EN)
Filing Language: English (EN)
Also published as:
AU1998072710