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1. WO2020234208 - PROCESS FOR THE PREPARATION OF GALNAC PHOSPHORAMIDITE EPIMERS

Publication Number WO/2020/234208
Publication Date 26.11.2020
International Application No. PCT/EP2020/063749
International Filing Date 18.05.2020
IPC
C07H 1/00 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
1Processes for the preparation of sugar derivatives
C07H 15/08 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
15Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
02Acyclic radicals, not substituted by cyclic structures
04attached to an oxygen atom of a saccharide radical
08Polyoxyalkylene derivatives
C07H 21/00 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
21Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids
CPC
C07H 1/00
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
1Processes for the preparation of sugar derivatives
C07H 15/08
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
15Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
02Acyclic radicals, not substituted by cyclic structures
04attached to an oxygen atom of the saccharide radical
08Polyoxyalkylene derivatives
C07H 21/00
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
21Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids
Applicants
  • F. HOFFMANN-LA ROCHE AG [CH]/[CH] (AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BE, BF, BG, BH, BJ, BN, BR, BW, BY, BZ, CA, CF, CG, CH, CI, CL, CM, CN, CO, CR, CU, CY, CZ, DE, DJ, DK, DM, DO, DZ, EC, EE, EG, ES, FI, FR, GA, GB, GD, GE, GH, GM, GN, GQ, GR, GT, GW, HN, HR, HU, ID, IE, IL, IN, IR, IS, IT, JO, JP, KE, KG, KH, KM, KN, KP, KR, KW, KZ, LA, LC, LK, LR, LS, LT, LU, LV, LY, MA, MC, MD, ME, MG, MK, ML, MN, MR, MT, MW, MX, MY, MZ, NA, NE, NG, NI, NL, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, SC, SD, SE, SG, SI, SK, SL, SM, SN, ST, SV, SY, SZ, TD, TG, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, UZ, VC, VN, WS, ZA, ZM, ZW)
  • HOFFMANN-LA ROCHE INC. [US]/[US] (US)
Inventors
  • BREITLER, Simon Adolf
  • PUENTENER, Kurt
Agents
  • RAUBER, Beat
Priority Data
19175309.420.05.2019EP
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) PROCESS FOR THE PREPARATION OF GALNAC PHOSPHORAMIDITE EPIMERS
(FR) PROCÉDÉ POUR LA PRÉPARATION D'ÉPIMÈRES DE PHOSPHORAMIDITE GALNAC
Abstract
(EN)
The invention comprises a process for the preparation of a GalNAc phosphoramidite epimer of the formula (I), wherein R1 is a hydroxy protecting group, n is an integer from 0 to 10 and m is an integer from 0 to 20, corresponding enantiomers and/ or optical isomers thereof and the use of the process for the preparation of GalNAc-cluster oligonucleotide conjugates.
(FR)
L'invention concerne un procédé de préparation d'un épimère de phosphoramidite GalNAc de Formule (I), dans laquelle R1 est un groupe protecteur hydroxy, n est un nombre entier de 0 à 10 et m est un nombre entier de 0 à 20, des énantiomères correspondants et/ou des isomères optiques de celui-ci et l'utilisation du procédé pour la préparation de conjugués oligonucléotidiques d'agrégats de GalNAc.
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