AU9442198A - Combined generation of phosphinic acid derivatives - Google Patents
Combined generation of phosphinic acid derivativesInfo
- Publication number
- AU9442198A AU9442198A AU94421/98A AU9442198A AU9442198A AU 9442198 A AU9442198 A AU 9442198A AU 94421/98 A AU94421/98 A AU 94421/98A AU 9442198 A AU9442198 A AU 9442198A AU 9442198 A AU9442198 A AU 9442198A
- Authority
- AU
- Australia
- Prior art keywords
- resin
- linker
- bound
- compounds
- acid derivatives
- Prior art date
- 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
Links
- ACVYVLVWPXVTIT-UHFFFAOYSA-N phosphinic acid Chemical class O[PH2]=O ACVYVLVWPXVTIT-UHFFFAOYSA-N 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 5
- 239000011347 resin Substances 0.000 abstract 5
- 229920005989 resin Polymers 0.000 abstract 5
- ACVYVLVWPXVTIT-UHFFFAOYSA-M phosphinate Chemical compound [O-][PH2]=O ACVYVLVWPXVTIT-UHFFFAOYSA-M 0.000 abstract 2
- 229920000642 polymer Polymers 0.000 abstract 2
- 239000000126 substance Substances 0.000 abstract 2
- 230000004071 biological effect Effects 0.000 abstract 1
- 239000003054 catalyst Substances 0.000 abstract 1
- 238000006243 chemical reaction Methods 0.000 abstract 1
- 238000001212 derivatisation Methods 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- XRBCRPZXSCBRTK-UHFFFAOYSA-N phosphonous acid Chemical class OPO XRBCRPZXSCBRTK-UHFFFAOYSA-N 0.000 abstract 1
- 238000002360 preparation method Methods 0.000 abstract 1
- 239000007790 solid phase Substances 0.000 abstract 1
- 238000006467 substitution reaction Methods 0.000 abstract 1
- 230000009897 systematic effect Effects 0.000 abstract 1
Classifications
-
- 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 Table
- C07F9/02—Phosphorus compounds
- C07F9/28—Phosphorus compounds with one or more P—C bonds
- C07F9/30—Phosphinic acids [R2P(=O)(OH)]; Thiophosphinic acids ; [R2P(=X1)(X2H) (X1, X2 are each independently O, S or Se)]
- C07F9/32—Esters thereof
- C07F9/3205—Esters thereof the acid moiety containing a substituent or a structure which is considered as characteristic
- C07F9/3229—Esters of aromatic acids (P-C aromatic linkage)
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C40—COMBINATORIAL TECHNOLOGY
- C40B—COMBINATORIAL CHEMISTRY; LIBRARIES, e.g. CHEMICAL LIBRARIES
- C40B40/00—Libraries per se, e.g. arrays, mixtures
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biochemistry (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Molecular Biology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Addition Polymer Or Copolymer, Post-Treatments, Or Chemical Modifications (AREA)
- Polyoxymethylene Polymers And Polymers With Carbon-To-Carbon Bonds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Other Resins Obtained By Reactions Not Involving Carbon-To-Carbon Unsaturated Bonds (AREA)
Abstract
Solid-phase-bound processes are disclosed for the systematic preparation of chemical compounds from the group of the phosphinic or phosphonous acids or their derivatives, and corresponding substance libraries which can be used for test purposes, in particular tests for biological effects. Compounds having the formula (I) YR<1>P(=O)(OR<3>)R<2>, in which Y, R<1>, R<2>, R<3> are defined as in Claim 1, are prepared by reacting a resin linker addition product (II) [resin polymer]-[linker-Z-E<1>-S<1>]n with a phosphinate (III) A<1>-O-(PHO)A*, in the presence of a suitable Pd catalyst, causing the substitution of group S<1> and yielding compound (IV) [resin polymer]-[linker-Z-E<1>-P(H)(=O)-OA<1>"], and after resin-bound derivatisation reactions, by separating the compound (I) from the resin-linker addition product. Also disclosed are the intermediate steps and resin-bound intermediate compounds, as well as the resultant substance libraries.
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US6161997P | 1997-10-09 | 1997-10-09 | |
| US60/061619 | 1997-10-09 | ||
| DE19745628A DE19745628A1 (en) | 1997-10-10 | 1997-10-10 | Solid-phase synthesis of aromatic phosphinic acid derivatives |
| DE19745628 | 1997-10-10 | ||
| PCT/EP1998/006162 WO1999019332A1 (en) | 1997-10-09 | 1998-09-29 | Combined generation of phosphinic acid derivatives |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| AU9442198A true AU9442198A (en) | 1999-05-03 |
| AU758910B2 AU758910B2 (en) | 2003-04-03 |
Family
ID=26040863
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AU94421/98A Ceased AU758910B2 (en) | 1997-10-09 | 1998-09-29 | Combined generation of phosphinic acid derivatives |
Country Status (9)
| Country | Link |
|---|---|
| EP (1) | EP1023299B1 (en) |
| JP (1) | JP2001519433A (en) |
| AT (1) | ATE215090T1 (en) |
| AU (1) | AU758910B2 (en) |
| CA (1) | CA2306076A1 (en) |
| DK (1) | DK1023299T3 (en) |
| ES (1) | ES2172206T3 (en) |
| IL (1) | IL135526A0 (en) |
| WO (1) | WO1999019332A1 (en) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ATE478083T1 (en) | 1999-03-05 | 2010-09-15 | Massachusetts Inst Technology | LINKER FOR THE SYNTHESIS OF OLIGOSACCHARIDES ON SOLID SUPPORTS |
| JP2006036701A (en) * | 2004-07-28 | 2006-02-09 | Ricoh Co Ltd | New solid phosphonate support, solid olefin support, method for producing the same and method for producing olefin compound using the same |
Family Cites Families (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE2346657A1 (en) * | 1973-09-17 | 1975-07-24 | Hoechst Ag | CARBOXYPHENYLALKYLPHOSPHIC ACIDS AND THEIR ESTERS AND PROCESS FOR THEIR PRODUCTION |
-
1998
- 1998-09-29 ES ES98947555T patent/ES2172206T3/en not_active Expired - Lifetime
- 1998-09-29 AT AT98947555T patent/ATE215090T1/en not_active IP Right Cessation
- 1998-09-29 JP JP2000515903A patent/JP2001519433A/en active Pending
- 1998-09-29 DK DK98947555T patent/DK1023299T3/en active
- 1998-09-29 CA CA002306076A patent/CA2306076A1/en not_active Abandoned
- 1998-09-29 IL IL13552698A patent/IL135526A0/en not_active IP Right Cessation
- 1998-09-29 WO PCT/EP1998/006162 patent/WO1999019332A1/en active IP Right Grant
- 1998-09-29 AU AU94421/98A patent/AU758910B2/en not_active Ceased
- 1998-09-29 EP EP98947555A patent/EP1023299B1/en not_active Expired - Lifetime
Also Published As
| Publication number | Publication date |
|---|---|
| EP1023299A1 (en) | 2000-08-02 |
| ATE215090T1 (en) | 2002-04-15 |
| CA2306076A1 (en) | 1999-04-22 |
| JP2001519433A (en) | 2001-10-23 |
| DK1023299T3 (en) | 2002-07-22 |
| IL135526A0 (en) | 2001-05-20 |
| ES2172206T3 (en) | 2002-09-16 |
| WO1999019332A1 (en) | 1999-04-22 |
| EP1023299B1 (en) | 2002-03-27 |
| AU758910B2 (en) | 2003-04-03 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| AU655164B2 (en) | Uncharged morpholino-based polymers having phosphorous-containing chiral intersubunit linkages | |
| US5948386A (en) | Conjugate and method for forming aminomethyl phosphorus conjugates | |
| Rivera et al. | Architectural chemistry: synthesis of topologically diverse macromulticycles by sequential multiple multicomponent macrocyclizations | |
| WO2001068583A3 (en) | Process for the carbonylation of ethylenically unsaturated compounds | |
| Dwars et al. | Synthesis of Optically Active α‐Amino‐phosphinic Acids by Catalytic Asymmetric Hydrogenation in Organic Solvents and Aqueous Micellar Media | |
| US6271315B1 (en) | Methods for making multivalent arrays | |
| Christensen et al. | Efficient Solid‐Phase Synthesis of Peptide‐Based Phosphine Ligands: Towards Combinatorial Libraries of Selective Transition Metal Catalysts | |
| Foust et al. | Stability and efficiency of mixed aryl phosphonate prodrugs | |
| Cao et al. | Direct Enamido C (sp2)− H Diphosphorylation Enabled by a PCET‐Triggered Double Radical Relay: Access to gem‐Bisphosphonates | |
| AU9442198A (en) | Combined generation of phosphinic acid derivatives | |
| EP1200484B1 (en) | Methods and reagents making multivalent arrays and combinatorial libraries of multivalent arrays | |
| Ito et al. | Tag‐Reporter and Resin Capture–Release Strategy in Oligosaccharide Synthesis | |
| Larsson et al. | Solid phase phosphorylation of a peptide by the H-phosphonate method | |
| Sbovata et al. | Synthesis and coordination of the bifunctionalized ylides Ph2P (CH2) n (Ph) 2PCHCOOMe (n= 1, 2) and ketenylidene Ph2P (CH2) 2 (Ph) 2PCCO to Pd and Pt complexes | |
| Desai et al. | Ligand discrimination in the reaction of nitrones with [PtCl 2 (PhCN) 2]. Selective formation of mono-oxadiazoline and mixed bis-oxadiazoline complexes under thermal and microwave conditions | |
| Kromm et al. | A new family of chelating diphosphines with transition-metal and carbon stereocenters in the backbone: A second-generation rhenium-containing system | |
| NO322888B1 (en) | Monofunctional EDTA, DTPA and TTHA derivatives, processes for their preparation and use thereof for the manufacture of medicaments | |
| Li | Synthesis of N-phosphoryl amino acid esters | |
| Chang et al. | Versatile fluorescence labeling method using activated esters on solid support | |
| MXPA01004672A (en) | Polynucleotide crosslinking agents. | |
| Ueki et al. | Phosphinyl and phosphinothioyl amino acids and peptides. VII. The use of the dimethylphosphinothioyl group as a thiol-protecting group of cysteine. | |
| WO1996023749A1 (en) | Chemical libraries, labelling and deconvolution thereof | |
| Lim et al. | Resolution and enantiomeric purities of [2-(methylsulfinyl) ethyl] amine | |
| Ballivet-Tkatchenko et al. | Cationic metal nitrosyl complexes. 6. Characterization of the 19-electron iron nitrosyl radical cation [Fe (NO) 2LL'2]+ | |
| Urnėžius et al. | Diphosphene and phosphoranylidenephosphine formation from a terminal phosphinidene complex |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FGA | Letters patent sealed or granted (standard patent) |