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1. WO2020140559 - 5-DEOXY-D-RIBOSE DERIVATIVE

Publication Number WO/2020/140559
Publication Date 09.07.2020
International Application No. PCT/CN2019/112065
International Filing Date 19.10.2019
IPC
A61K 31/7068 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
70Carbohydrates; Sugars; Derivatives thereof
7042Compounds having saccharide radicals and heterocyclic rings
7052having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
706containing six-membered rings with nitrogen as a ring hetero atom
7064containing condensed or non-condensed pyrimidines
7068having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
C07H 13/12 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
13Compounds containing saccharide radicals esterified by carbonic acid or derivatives thereof, or by organic acids, e.g. phosphonic acids
12by acids having the group -X-C (=X)-X-, or halides thereof, in which X means nitrogen, oxygen, sulfur, selenium, or tellurium, e.g. carbonic acid, carbamic acid
C07H 19/06 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
19Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro derivatives thereof
02sharing nitrogen
04Heterocyclic radicals containing only nitrogen as ring hetero atom
06Pyrimidine radicals
C07H 1/00 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
1Processes for the preparation of sugar derivatives
A61P 35/00 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
CPC
A61K 31/7068
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
70Carbohydrates; Sugars; Derivatives thereof
7042Compounds having saccharide radicals and heterocyclic rings
7052having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
706containing six-membered rings with nitrogen as a ring hetero atom
7064containing condensed or non-condensed pyrimidines
7068having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
A61P 35/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
C07H 1/00
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
1Processes for the preparation of sugar derivatives
C07H 13/12
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
13Compounds containing saccharide radicals esterified by carbonic acid or derivatives thereof, or by organic acids, e.g. phosphonic acids
12by acids having the group -X-C(=X)-X-, or halides thereof, in which each X means nitrogen, oxygen, sulfur, selenium or tellurium, e.g. carbonic acid, carbamic acid
C07H 19/06
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
19Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides ; Anhydro-derivatives thereof
02sharing nitrogen
04Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
06Pyrimidine radicals
C07H 3/08
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
3Compounds containing only hydrogen atoms and saccharide radicals having only carbon, hydrogen, and oxygen atoms
08Deoxysugars; Unsaturated sugars
Applicants
  • 鲁南制药集团股份有限公司 LUNAN PHARMACEUTICAL GROUP CORPORATION
Inventors
  • 张贵民 ZHANG, Guimin
  • 白文钦 BAI, Wenqin
  • 郑艺 ZHENG, Yi
Priority Data
201811648376.830.12.2018CN
Publication Language Chinese (ZH)
Filing Language Chinese (ZH)
Designated States
Title
(EN) 5-DEOXY-D-RIBOSE DERIVATIVE
(FR) DÉRIVÉ DU 5-DÉSOXY-D-RIBOSE
(ZH) 一种5-脱氧-D-核糖衍生物
Abstract
(EN)
Provided is a 5-deoxy-D-ribose derivative (III), when the derivative (III) is used for preparing capecitabine, the stereoselectivity is good and the yield is high. Further provided is a preparation method of the derivative, wherein the preparation method comprises: step a: performing oxymethylation of 1-hydroxyl group of 5-deoxy-D-ribose; step b: protecting 2-, 3-hydroxyl groups with Fmoc-; and finally protecting the 1-group with acetylation. The method is simple and convenient to operate, does not need special equipment, and is suitable for industrial production.
(FR)
L'invention concerne un dérivé du 5-désoxy-D-ribose (III), qui, lors de l'utilisation de ce dérivé (III) pour préparer de la capécitabine, permet une bonne stéréosélectivité et un rendement élevé. L'invention concerne en outre un procédé de préparation du dérivé, le procédé de préparation comprenant : une étape a, consistant à réaliser une oxyméthylation du groupe 1-hydroxyl du 5-désoxy-D-ribose ; une étape b, consistant à protéger les groupes 2-, 3-hydroxyl avec du Fmoc- ; et enfin une étape consistant à protéger le groupe 1 par acétylation. Le procédé est simple et pratique à utiliser, ne nécessite pas d'équipement spécial, et est approprié pour une production industrielle.
(ZH)
提供了一种 5-脱氧-D-核糖衍生物(III),使用该衍生物(III)制备卡培他滨时,立体选择性好,收率高。还提供了一种该衍生物的制备方法,其制备方法包括:步骤 a:5-脱氧-D-核糖 1 位羟基的氧甲基化;步骤 b:2,3 位羟基用 Fmoc-进行保护;最后对 1 位用乙酰化进行保护。该方法操作简便,不需要特殊设备,适合工业化生产。
Also published as
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