AU3275684A

AU3275684A – Preparation of phosphorus-containing nucleoside derivatives
– Google Patents

AU3275684A – Preparation of phosphorus-containing nucleoside derivatives
– Google Patents
Preparation of phosphorus-containing nucleoside derivatives

Info

Publication number
AU3275684A

AU3275684A
AU32756/84A
AU3275684A
AU3275684A
AU 3275684 A
AU3275684 A
AU 3275684A
AU 32756/84 A
AU32756/84 A
AU 32756/84A
AU 3275684 A
AU3275684 A
AU 3275684A
AU 3275684 A
AU3275684 A
AU 3275684A
Authority
AU
Australia
Prior art keywords
denotes
general formula
see diagramm
given above
meanings given
Prior art date
1983-09-06
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)

Granted

Application number
AU32756/84A
Other versions

AU570266B2
(en

Inventor
Joachim Engels
Alfred Jager
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)

Hoechst AG

Original Assignee
Hoechst AG
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
1983-09-06
Filing date
1984-09-05
Publication date
1985-03-14

1984-09-05
Application filed by Hoechst AG
filed
Critical
Hoechst AG

1985-03-14
Publication of AU3275684A
publication
Critical
patent/AU3275684A/en

1988-03-10
Application granted
granted
Critical

1988-03-10
Publication of AU570266B2
publication
Critical
patent/AU570266B2/en

2004-09-05
Anticipated expiration
legal-status
Critical

Status
Expired
legal-status
Critical
Current

Links

Espacenet

Global Dossier

Discuss

Classifications

C—CHEMISTRY; METALLURGY

C07—ORGANIC CHEMISTRY

C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS

C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof

C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen

C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom

C—CHEMISTRY; METALLURGY

C07—ORGANIC CHEMISTRY

C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM

C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic System

C07F9/02—Phosphorus compounds

C07F9/28—Phosphorus compounds with one or more P—C bonds

C07F9/48—Phosphonous acids R—P(OH)2; Thiophosphonous acids including RHP(=O)(OH); Derivatives thereof

C07F9/4883—Amides or esteramides thereof, e.g. RP(NR’2)2 or RP(XR’)(NR»2) (X = O, S)

C—CHEMISTRY; METALLURGY

C07—ORGANIC CHEMISTRY

C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS

C07H21/00—Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids

Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS

Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE

Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS

Y02P20/00—Technologies relating to chemical industry

Y02P20/50—Improvements relating to the production of bulk chemicals

Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

Abstract

1. Claims for the contracting states : BE, CH, LI, DE, FR, GB, IT, LU, NL, SE A process for the preparation of deoxyribonucleoside phosphonates of the general formula I see diagramm : EP0136543,P14,F1 in which T denotes a protecting group for a primary hydroxyl group, B denotes a nucleoside base radical in which any exoamino group present is protected, G denotes a protecting group for a secondary hydroxyl group, Z denotes oxygen, sulfur or selenium and R denotes alkyl having up to 8 C atoms, cyclohexyl, benzyl, or phenyl which is optionally substituted by fluorine, chlorine, bromine, lower alkyl, lower alkoxy or trifluoromethyl, characterized in that a difunctional phosphonylating reagent of the general formula II see diagramm : EP0136543,P14,F2 in which X denotes chlorine or Y and Y denotes a group of the formula see diagramm : EP0136543,P14,F3 R**1 and R**2 representing identical or different alkyl or cycloalkyl radicals having up to 8 C atoms, or phenyl radicals, or R**1 and R**2 , together with the nitrogen, representing a saturated or unsaturated heterocyclic ring which can contain further hetero atoms, being reacted with a nucleoside of the general formula III see diagramm : EP0136543,P14,F4 in which T and B have the meanings given above, the resulting compound of the general formula IV see diagramm : EP0136543,P14,F5 being reacted with a compound of the general formula V see diagramm : EP0136543,P15,F1 in which B and G have the meanings given above, and the resulting compounds of the general formula VI see diagramm : EP0136543,P15,F2 in which T, R, B and G have the meanings given above, being oxidatively converted to compound of the general formula I. 1. Claims for the contracting state AT A process for the preparation of deoxyribonucleoside phosphonates of the general formula I see diagramm : EP0136543,P15,F3 in which T denotes a protecting group for a primary hydroxyl group, B denotes a nucleoside base radical in which any exoamino group present is protected, G denotes a protecting group for a secondary hydroxyl group, Z denotes oxygen, sulfur or selenium and R denotes alkyl having up to 8 C atoms, cyclohexyl, benzyl, or phenyl which is optionally substituted by fluorine, chlorine, bromine, lower alkyl, lower alkoxy or trifluoromethyl, characterized in that a difunctional phosphonylating reagent of the general formula II see diagramm : EP0136543,P16,F1 in which X denotes chlorine or Y and Y denotes a group of the formula see diagramm : EP0136543,P16,F2 R**1 and R**2 representing identical or different alkyl or cycloalkyl radicals having up to 8 C atoms, or phenyl radicals, or R**1 and R**2 , together with the nitrogen, representing a saturated or unsaturated heterocyclic ring which can contain further hetero atoms, being reacted with a nucleoside of the general formula III see diagramm : EP0136543,P16,F3 in which T and B have the meanings given above, the resulting compound of the general formula IV see diagramm : EP0136543,P16,F4 being reacted with a compound of the general formula V see diagramm : EP0136543,P16,F5 in which B and G have the meanings given above, and the resulting compounds of the general formula VI see diagramm : EP0136543,P17,F1 in which T, R, B and G have the meanings given above, being oxidatively converted to compound of the general formula I.

AU32756/84A
1983-09-06
1984-09-05
Preparation of phosphorus-containing nucleoside derivatives

Expired

AU570266B2
(en)

Applications Claiming Priority (2)

Application Number
Priority Date
Filing Date
Title

DE3332068

1983-09-06

DE19833332068

DE3332068A1
(en)

1983-09-06
1983-09-06

METHOD FOR PRODUCING NUCLEOSIDALKYL, ARALKYL AND ARYLPHOSPHONITES AND PHOSPHONATES

Related Child Applications (1)

Application Number
Title
Priority Date
Filing Date

AU11384/88A
Division

AU601257B2
(en)

1983-09-06
1988-02-08
5′-protected nucleoside phosphonites and process for their preparation

Publications (2)

Publication Number
Publication Date

AU3275684A
true

AU3275684A
(en)

1985-03-14

AU570266B2

AU570266B2
(en)

1988-03-10

Family
ID=6208339
Family Applications (2)

Application Number
Title
Priority Date
Filing Date

AU32756/84A
Expired

AU570266B2
(en)

1983-09-06
1984-09-05
Preparation of phosphorus-containing nucleoside derivatives

AU11384/88A
Expired

AU601257B2
(en)

1983-09-06
1988-02-08
5′-protected nucleoside phosphonites and process for their preparation

Family Applications After (1)

Application Number
Title
Priority Date
Filing Date

AU11384/88A
Expired

AU601257B2
(en)

1983-09-06
1988-02-08
5′-protected nucleoside phosphonites and process for their preparation

Country Status (11)

Country
Link

EP
(1)

EP0136543B1
(en)

JP
(2)

JPS6072899A
(en)

AT
(1)

ATE38839T1
(en)

AU
(2)

AU570266B2
(en)

CA
(1)

CA1235079A
(en)

DE
(2)

DE3332068A1
(en)

DK
(3)

DK162895C
(en)

ES
(1)

ES8505384A1
(en)

GR
(1)

GR80287B
(en)

IE
(1)

IE57904B1
(en)

PT
(1)

PT79172B
(en)

Cited By (1)

* Cited by examiner, † Cited by third party

Publication number
Priority date
Publication date
Assignee
Title

US4959463A
(en)

*

1985-10-15
1990-09-25
Genentech, Inc.
Intermediates

Families Citing this family (12)

* Cited by examiner, † Cited by third party

Publication number
Priority date
Publication date
Assignee
Title

DE3916871A1
(en)

*

1989-05-24
1990-11-29
Boehringer Mannheim Gmbh

MODIFIED PHOSPHORAMIDITE PROCESS FOR THE PREPARATION OF MODIFIED NUCLEIC ACIDS

DE59108644D1
(en)

*

1990-07-02
1997-05-07
Hoechst Ag

Oligonucleotide analogs with terminal 3′-3 ‘or. 5’-5 ‘internucleotide linkages

US5512668A
(en)

*

1991-03-06
1996-04-30
Polish Academy Of Sciences
Solid phase oligonucleotide synthesis using phospholane intermediates

WO1994002499A1
(en)

*

1992-07-27
1994-02-03
Hybridon, Inc.
Oligonucleotide alkylphosphonothioates

US6087491A
(en)

*

1993-01-08
2000-07-11
Hybridon, Inc.
Extremely high purity oligonucleotides and methods of synthesizing them using dimer blocks

ES2100051T3
(en)

*

1993-01-08
1997-06-01
Hybridon Inc

SYNTHESIS OF DIMER BLOCKS AND THEIR USE IN THE ASSEMBLY OF OLIGONUCLEOTIDES.

AU6165494A
(en)

*

1993-01-25
1994-08-15
Hybridon, Inc.
Oligonucleotide alkylphosphonates and alkylphosphonothioates

DE69527266T2
(en)

*

1994-07-26
2003-03-06
Sony Corp

IMAGE TRANSFER METHOD

PT828749E
(en)

*

1995-05-26
2003-11-28
Genta Inc

COMPOSITIONS AND METHODS FOR SYNTHESIS OF ORGANOPHOSPHORUS DERIVATIVES

CA2226111C
(en)

*

1996-05-03
2005-09-20
Hybridon, Inc.
In situ preparation of nucleoside phosphoramidites and their use in synthesis of oligonucleotides

DE102004049339A1
(en)

2004-10-08
2006-04-13
Basf Ag

Process for the purification of phosphorus-containing chelate ligands

DE102007038930B4
(en)

*

2007-08-13
2013-12-05
Universität Leipzig

New chemical compound and its use in medicine, in particular for use in tumor therapy

Family Cites Families (4)

* Cited by examiner, † Cited by third party

Publication number
Priority date
Publication date
Assignee
Title

IL62834A0
(en)

*

1980-05-14
1981-07-31
Ens Bio Logicals Inc
Polynucleotide synthesis

US4415732A
(en)

*

1981-03-27
1983-11-15
University Patents, Inc.
Phosphoramidite compounds and processes

EP0090789A1
(en)

*

1982-03-26
1983-10-05
Monsanto Company
Chemical DNA synthesis

DE3239888A1
(en)

*

1982-10-28
1984-05-03
Hubert Prof. Dr. 2000 Hamburg Köster

METHOD FOR PRODUCING OLIGONUCLEOSIDE PHOSPHONATES

1983

1983-09-06
DE
DE19833332068
patent/DE3332068A1/en
not_active
Withdrawn

1984

1984-08-30
AT
AT84110314T
patent/ATE38839T1/en
not_active
IP Right Cessation

1984-08-30
DE
DE8484110314T
patent/DE3475307D1/en
not_active
Expired

1984-08-30
EP
EP84110314A
patent/EP0136543B1/en
not_active
Expired

1984-09-04
GR
GR80287A
patent/GR80287B/en
unknown

1984-09-04
PT
PT79172A
patent/PT79172B/en
active
IP Right Revival

1984-09-04
ES
ES535627A
patent/ES8505384A1/en
not_active
Expired

1984-09-05
AU
AU32756/84A
patent/AU570266B2/en
not_active
Expired

1984-09-05
JP
JP59184717A
patent/JPS6072899A/en
active
Granted

1984-09-05
IE
IE2268/84A
patent/IE57904B1/en
not_active
IP Right Cessation

1984-09-05
DK
DK424784A
patent/DK162895C/en
active

1984-09-05
CA
CA000462469A
patent/CA1235079A/en
not_active
Expired

1988

1988-02-08
AU
AU11384/88A
patent/AU601257B2/en
not_active
Expired

1991

1991-07-05
DK
DK131691A
patent/DK167359B1/en
active
IP Right Grant

1991-07-05
DK
DK131591A
patent/DK166585C/en
active

1992

1992-11-18
JP
JP4307481A
patent/JPH0662662B2/en
not_active
Expired – Fee Related

Cited By (1)

* Cited by examiner, † Cited by third party

Publication number
Priority date
Publication date
Assignee
Title

US4959463A
(en)

*

1985-10-15
1990-09-25
Genentech, Inc.
Intermediates

Also Published As

Publication number
Publication date

DK166585B
(en)

1993-06-14

AU570266B2
(en)

1988-03-10

GR80287B
(en)

1985-01-07

IE842268L
(en)

1985-03-06

PT79172A
(en)

1984-10-01

DK131591D0
(en)

1991-07-05

CA1235079A
(en)

1988-04-12

DK162895B
(en)

1991-12-23

DK424784A
(en)

1985-03-07

JPH0531560B2
(en)

1993-05-12

DK166585C
(en)

1993-10-25

JPH0662662B2
(en)

1994-08-17

PT79172B
(en)

1986-09-10

EP0136543A2
(en)

1985-04-10

JPH05262787A
(en)

1993-10-12

DE3332068A1
(en)

1985-03-21

EP0136543A3
(en)

1986-07-16

AU601257B2
(en)

1990-09-06

DK131691A
(en)

1991-07-05

ES535627A0
(en)

1985-05-16

AU1138488A
(en)

1988-07-14

JPS6072899A
(en)

1985-04-24

DK131591A
(en)

1991-07-05

DK131691D0
(en)

1991-07-05

ATE38839T1
(en)

1988-12-15

DK424784D0
(en)

1984-09-05

IE57904B1
(en)

1993-05-05

DK162895C
(en)

1992-05-11

DK167359B1
(en)

1993-10-18

DE3475307D1
(en)

1988-12-29

ES8505384A1
(en)

1985-05-16

EP0136543B1
(en)

1988-11-23

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