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1. (JP2001097973 ) ENANTIOMERICALLY PURE -D-(-)-dioxolane-nucleoside

Office : Japan
Application Number: 2000246125 Application Date: 15.08.2000
Publication Number: 2001097973 Publication Date: 10.04.2001
Grant Number: 3881165 Grant Date: 14.02.2007
Publication Kind : B2
IPC:
C07D 405/4
C07D 473/18
A61K 31/505
A61K 31/506
A61K 31/513
A61K 31/52
A61K 31/522
A61K 31/53
A61K 31/675
A61K 31/7076
A61P 31/12
A61P 31/18
A61P 37/4
C07D 327/4
C07D 411/4
C07D 473/0
C07D 473/30
C07D 473/34
C07D 473/40
C07D 497/8
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
405
Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
02
containing two hetero rings
04
directly linked by a ring-member-to-ring- member bond
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
473
Heterocyclic compounds containing purine ring systems
02
with oxygen, sulfur, or nitrogen atoms directly attached in positions 2 and 6
18
one oxygen and one nitrogen atom, e.g. guanine
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
495
having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
505
Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
495
having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
505
Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
506
not condensed and containing further heterocyclic rings
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
495
having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
505
Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
513
having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
495
having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
505
Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
519
ortho- or peri-condensed with heterocyclic rings
52
Purines, e.g. adenine
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
495
having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
505
Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
519
ortho- or peri-condensed with heterocyclic rings
52
Purines, e.g. adenine
522
having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
53
having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
66
Phosphorus compounds
675
having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
70
Carbohydrates; Sugars; Derivatives thereof
7042
Compounds having saccharide radicals and heterocyclic rings
7052
having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
706
containing six-membered rings with nitrogen as a ring hetero atom
7064
containing condensed or non-condensed pyrimidines
7076
containing purines, e.g. adenosine, adenylic acid
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
31
Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
12
Antivirals
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
31
Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
12
Antivirals
14
for RNA viruses
18
for HIV
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
37
Drugs for immunological or allergic disorders
02
Immunomodulators
04
Immunostimulants
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
327
Heterocyclic compounds containing rings having oxygen and sulfur atoms as the only ring hetero atoms
02
one oxygen atom and one sulfur atom
04
Five-membered rings
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
411
Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen and sulfur atoms as the only ring hetero atoms
02
containing two hetero rings
04
directly linked by a ring-member-to-ring- member bond
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
473
Heterocyclic compounds containing purine ring systems
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
473
Heterocyclic compounds containing purine ring systems
26
with an oxygen, sulfur, or nitrogen atom directly attached in position 2 or 6, but not in both
28
Oxygen atom
30
attached in position 6, e.g. hypoxanthine
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
473
Heterocyclic compounds containing purine ring systems
26
with an oxygen, sulfur, or nitrogen atom directly attached in position 2 or 6, but not in both
32
Nitrogen atom
34
attached in position 6, e.g. adenine
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
473
Heterocyclic compounds containing purine ring systems
40
with halogen atoms or perhalogeno-alkyl radicals directly attached in position 2 or 6
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
497
Heterocyclic compounds containing in the condensed system at least one hetero ring having oxygen and sulfur atoms as the only ring hetero atoms
02
in which the condensed system contains two hetero rings
08
Bridged systems
Applicants: UNIV OF GEORGIA RESEARCH FOUNDATION INC
ユニバーシティ・オブ・ジョージア・リサーチ・ファウンデイション・インコーポレイテッド; アメリカ合衆国30602-7411ジョージア州アセンズ、ボイド・グラデュエイト・スタディーズ・リサーチ・センター
UNIV EMORY
エモリー・ユニバーシテイ; アメリカ合衆国、ジヨージア・30322、アトランタ、サウス・オツクスフオード・ロード・1380
Inventors: CHU CHUNG K
チュン,ケイ.チュウ
SCHINAZI RAYMOND F
レイモンド,エフ.シナッツィ
Priority Data: 07622762 05.12.1990 US
Title: (EN) ENANTIOMERICALLY PURE -D-(-)-dioxolane-nucleoside
(JA) 鏡像異性的に純粋なβ-D-(-)-ジオキソラン-ヌクレオシド
Abstract:
(EN) PROBLEM TO BE SOLVED: To provide a method for producing a compound having high HIV activity.

SOLUTION: A process for the preparation of enantiomerically pure -D-(-)- dxoxolane-nucleosides (e.g. a compound represented by formula 2 when thymine is used as a base) comprises a step for preparing a dioxolane ring from 1,6- anhydromannose represented by formula 1. The base is selected from adenine, hypoxanthine, cytosine, uracil, etc., in addition to thymine.

COPYRIGHT: (C)2001,JPO
(JA)


(修正有)


【課題】 HIV活性の高い化合物の製造方法の提供。


【解決手段】 式1で示される1,6-アンヒドロマン
ノースからジオキソラン環を調製する工程を含む、鏡像
異性的に純粋なβ-D-(-)-ジオキソラン-ヌクレ
オシド(例えば塩基としてチミンを用いる場合は、式2
で示される化合物)調製のためのプロセス。
塩基として
はチミンの他に、アデニン、ヒポキサンチン、シトシ
ン、ウラシル等から選ばれる。


Also published as:
ES2291268EP0562009JP2007008959US5925643JP3421335JPH07502973
CA2099589CA2590125AU1991091259AU1991091475AU1997016640WO/1992/010497