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1. WO2022006871 - PROCESSES FOR PREPARING OLIGONUCLEOTIDES

Publication Number WO/2022/006871
Publication Date 13.01.2022
International Application No. PCT/CN2020/101401
International Filing Date 10.07.2020
IPC
C07D 487/04 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
487Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/-C07D477/183
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
C07D 519/00 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
519Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/ or C07D455/257
Applicants
  • CHANGZHOU SYNTHEALL PHARMACEUTICALS CO., LTD. [CN]/[CN]
  • SHANGHAI STA PHARMACEUTICAL R&D CO., LTD. [CN]/[CN]
Inventors
  • HU, Chenchen
  • ZHAO, Qiang
  • LI, Qing
  • YANG, Jimin
Agents
  • SHANGHAI BESHINING LAW OFFICE
Priority Data
Publication Language English (en)
Filing Language English (EN)
Designated States
Title
(EN) PROCESSES FOR PREPARING OLIGONUCLEOTIDES
(FR) PROCÉDÉS DE PRÉPARATION D’OLIGONUCLÉOTIDES
Abstract
(EN) Disclosed are processes for preparing oligonucleotides. The process comprises: (a) converting a compound of Formula X-1 into a compound of Formula X-2: where R10 is a residue of an oligonucleotide (e.g., a phosphorodiamidate morpholino oligomer); R11 is an amine protecting group; wherein the compound of Formula X-1 is not bound to a solid support; and; (b) optionally removing protecting groups in the compound of Formula X-2 to obtain the oligonucleotide. The synthetic processes described herein are advantageous in many aspects, including but not limited to improved yields and purities of target phosphorodiamidate morpholino oligomers with reduced 4-nitrostyrene adduct impurities. (X-1), (X-2)
(FR) L’invention divulgue des procédés de préparation d’oligonucléotides. Le procédé comprend : (a) la conversion d’un composé de Formule X-1 en un composé de Formule X-2 : dans lesquelles R10 représentent un résidu d’un oligonucléotide (par exemple, un oligomère de phosphorodiamidate morpholino) ; R11 représente un groupe protecteur d’amine ; le composé de Formule X-1 n’étant pas lié à un support solide ; et (b) éventuellement l’élimination des groupes protecteurs du composé de Formule X-2 pour obtenir l’oligonucléotide. Les procédés de synthèse décrits dans l'invention sont avantageux selon de nombreux aspects, comprenant, mais sans y être limités, des rendements et des puretés améliorés d'oligomères de phosphorodiamétylmorpholino cibles contenant des quantités réduites d'impuretés d'adduit de 4-nitrostyrène. (X-1), (X-2)
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