ES2068321T3 - La preparacion diastereoselectiva de esteres fosfinato. - Google Patents
La preparacion diastereoselectiva de esteres fosfinato.Info
- Publication number
- ES2068321T3 ES2068321T3 ES90125061T ES90125061T ES2068321T3 ES 2068321 T3 ES2068321 T3 ES 2068321T3 ES 90125061 T ES90125061 T ES 90125061T ES 90125061 T ES90125061 T ES 90125061T ES 2068321 T3 ES2068321 T3 ES 2068321T3
- Authority
- ES
- Spain
- Prior art keywords
- chem
- reaction
- formula
- resulting
- phosphinate esters
- 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.)
- Expired - Lifetime
Links
- ACVYVLVWPXVTIT-UHFFFAOYSA-M phosphinate Chemical class [O-][PH2]=O ACVYVLVWPXVTIT-UHFFFAOYSA-M 0.000 title 1
- -1 phosphinic acid ester Chemical class 0.000 abstract 3
- SJRJJKPEHAURKC-UHFFFAOYSA-N N-Methylmorpholine Chemical compound CN1CCOCC1 SJRJJKPEHAURKC-UHFFFAOYSA-N 0.000 abstract 2
- UUUHXMGGBIUAPW-UHFFFAOYSA-N 1-[1-[2-[[5-amino-2-[[1-[5-(diaminomethylideneamino)-2-[[1-[3-(1h-indol-3-yl)-2-[(5-oxopyrrolidine-2-carbonyl)amino]propanoyl]pyrrolidine-2-carbonyl]amino]pentanoyl]pyrrolidine-2-carbonyl]amino]-5-oxopentanoyl]amino]-3-methylpentanoyl]pyrrolidine-2-carbon Chemical compound C1CCC(C(=O)N2C(CCC2)C(O)=O)N1C(=O)C(C(C)CC)NC(=O)C(CCC(N)=O)NC(=O)C1CCCN1C(=O)C(CCCN=C(N)N)NC(=O)C1CCCN1C(=O)C(CC=1C2=CC=CC=C2NC=1)NC(=O)C1CCC(=O)N1 UUUHXMGGBIUAPW-UHFFFAOYSA-N 0.000 abstract 1
- NFDXQGNDWIPXQL-UHFFFAOYSA-N 1-cyclooctyldiazocane Chemical compound C1CCCCCCC1N1NCCCCCC1 NFDXQGNDWIPXQL-UHFFFAOYSA-N 0.000 abstract 1
- AVFZOVWCLRSYKC-UHFFFAOYSA-N 1-methylpyrrolidine Chemical compound CN1CCCC1 AVFZOVWCLRSYKC-UHFFFAOYSA-N 0.000 abstract 1
- 102000004270 Peptidyl-Dipeptidase A Human genes 0.000 abstract 1
- 108090000882 Peptidyl-Dipeptidase A Proteins 0.000 abstract 1
- 229940030600 antihypertensive agent Drugs 0.000 abstract 1
- 239000002220 antihypertensive agent Substances 0.000 abstract 1
- KMPWYEUPVWOPIM-KODHJQJWSA-N cinchonidine Chemical compound C1=CC=C2C([C@H]([C@H]3[N@]4CC[C@H]([C@H](C4)C=C)C3)O)=CC=NC2=C1 KMPWYEUPVWOPIM-KODHJQJWSA-N 0.000 abstract 1
- KMPWYEUPVWOPIM-UHFFFAOYSA-N cinchonidine Natural products C1=CC=C2C(C(C3N4CCC(C(C4)C=C)C3)O)=CC=NC2=C1 KMPWYEUPVWOPIM-UHFFFAOYSA-N 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 239000012973 diazabicyclooctane Substances 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 229960001880 fosinopril sodium Drugs 0.000 abstract 1
- 238000001640 fractional crystallisation Methods 0.000 abstract 1
- 230000005764 inhibitory process Effects 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 125000006239 protecting group Chemical group 0.000 abstract 1
- SBYHFKPVCBCYGV-UHFFFAOYSA-N quinuclidine Chemical compound C1CC2CCN1CC2 SBYHFKPVCBCYGV-UHFFFAOYSA-N 0.000 abstract 1
- TVTJZMHAIQQZTL-WATAJHSMSA-M sodium;(2s,4s)-4-cyclohexyl-1-[2-[[(1s)-2-methyl-1-propanoyloxypropoxy]-(4-phenylbutyl)phosphoryl]acetyl]pyrrolidine-2-carboxylate Chemical compound [Na+].C([P@@](=O)(O[C@H](OC(=O)CC)C(C)C)CC(=O)N1[C@@H](C[C@H](C1)C1CCCCC1)C([O-])=O)CCCC1=CC=CC=C1 TVTJZMHAIQQZTL-WATAJHSMSA-M 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
-
- 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
- C07F9/3258—Esters thereof the ester moiety containing a substituent or a structure which is considered as characteristic
- C07F9/3264—Esters with hydroxyalkyl compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/12—Antihypertensives
-
- 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
- C07F9/3211—Esters of acyclic saturated acids which can have further substituents on alkyl
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Biochemistry (AREA)
- Molecular Biology (AREA)
- General Chemical & Material Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Peptides Or Proteins (AREA)
- Cosmetics (AREA)
- Preparation Of Compounds By Using Micro-Organisms (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
Abstract
SE CONSIGUE UN INCREMENTO EN LA DIASTEREOSELECTIVIDAD RESULTANTE DE LA REACCION DE UN ESTER DEL ACIDO FOSFINICO DE LA FORMULA CON EL HALO DEL ESTER DE LA FORMULA PRODUCIENDO LA REACCION EN PRESENCIA DE 4-METILMORFOLINA, DIAZABICICLOOCTANO, QUINUCLIDINA, 1-METILPIROLIDINA O CINCONIDINA. DESPUES DE QUITAR EL GRUPO PROTECTOR R SUB 3 Y LA FRACCION DE LA CRISTALIZACION, EL PAR DIASTEREOMERICO DESEADO QUE RESULTA, ASI COMO EL ISOMERO DESEADO, PUEDEN SER EMPAREJADOS A LA 4-1-PROLINA SUSTITUIDA PARA DAR COMPUESTOS QUE TIENEN LA CAPACIDAD PARA INHIBIR LA ACTIVIDAD DE LA ENZIMA CONVERTIDORA DE LA ANGIOTENSINA. EN PARTICULAR, EL PROCESO ES UTIL PARA AUMENTAR LA PRODUCCION DEL AGENTE ANTIHIPERTENSIVO FOSINOPRILO SODICO.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US07/467,451 US5008399A (en) | 1990-01-19 | 1990-01-19 | Diastereoselective preparation of phosphinate esters |
Publications (1)
Publication Number | Publication Date |
---|---|
ES2068321T3 true ES2068321T3 (es) | 1995-04-16 |
Family
ID=23855753
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ES90125061T Expired - Lifetime ES2068321T3 (es) | 1990-01-19 | 1990-12-21 | La preparacion diastereoselectiva de esteres fosfinato. |
Country Status (19)
Country | Link |
---|---|
US (1) | US5008399A (es) |
EP (1) | EP0437799B1 (es) |
JP (1) | JP2846484B2 (es) |
KR (2) | KR0179368B1 (es) |
CN (1) | CN1026791C (es) |
AT (1) | ATE118779T1 (es) |
AU (1) | AU623562B2 (es) |
CA (1) | CA2032900C (es) |
DE (1) | DE69017183T2 (es) |
DK (1) | DK0437799T3 (es) |
ES (1) | ES2068321T3 (es) |
FI (1) | FI101539B1 (es) |
HU (1) | HU208142B (es) |
IE (1) | IE67354B1 (es) |
IL (1) | IL96838A (es) |
NO (1) | NO179915C (es) |
PT (1) | PT96519B (es) |
RU (1) | RU2044740C1 (es) |
ZA (1) | ZA9196B (es) |
Families Citing this family (7)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
GB9304619D0 (en) * | 1993-03-06 | 1993-04-21 | Ciba Geigy Ag | Esters |
US6555139B2 (en) | 1999-06-28 | 2003-04-29 | Wockhardt Europe Limited | Preparation of micron-size pharmaceutical particles by microfluidization |
JP2004520440A (ja) * | 2001-04-30 | 2004-07-08 | ルピン ラボラトリーズ リミティド | フォシノプリルナトリウムの製造方法 |
CN100497335C (zh) * | 2005-10-27 | 2009-06-10 | 上海医药工业研究院 | 取代氧膦基乙酸的光学拆分方法 |
CN100488969C (zh) * | 2005-10-27 | 2009-05-20 | 上海医药工业研究院 | 光学活性的取代氧膦基乙酸盐及其用途 |
IT1394407B1 (it) | 2009-05-25 | 2012-06-15 | Dipharma Francis Srl | Procedimento per la preparazione di fosinopril e suoi intermedi |
IT1406151B1 (it) | 2010-12-06 | 2014-02-14 | Dipharma Francis Srl | Procedimento per la preparazione di fosinopril e suoi intermedi |
Family Cites Families (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US4337201A (en) * | 1980-12-04 | 1982-06-29 | E. R. Squibb & Sons, Inc. | Phosphinylalkanoyl substituted prolines |
US4384123A (en) * | 1980-12-04 | 1983-05-17 | E. R. Squibb & Sons, Inc. | Phosphinylalkanoyl substituted prolines |
US4873356A (en) * | 1987-09-30 | 1989-10-10 | E. R. Squibb & Sons, Inc. | Method for preparing phosphinic acids used in preparing ace inhibitors and intermediates produced thereby |
-
1990
- 1990-01-19 US US07/467,451 patent/US5008399A/en not_active Expired - Lifetime
- 1990-12-20 AU AU68319/90A patent/AU623562B2/en not_active Expired
- 1990-12-20 CA CA002032900A patent/CA2032900C/en not_active Expired - Lifetime
- 1990-12-21 ES ES90125061T patent/ES2068321T3/es not_active Expired - Lifetime
- 1990-12-21 EP EP90125061A patent/EP0437799B1/en not_active Expired - Lifetime
- 1990-12-21 DK DK90125061.3T patent/DK0437799T3/da active
- 1990-12-21 AT AT90125061T patent/ATE118779T1/de not_active IP Right Cessation
- 1990-12-21 DE DE69017183T patent/DE69017183T2/de not_active Expired - Lifetime
- 1990-12-31 IL IL9683890A patent/IL96838A/en not_active IP Right Cessation
-
1991
- 1991-01-04 ZA ZA9196A patent/ZA9196B/xx unknown
- 1991-01-07 IE IE4791A patent/IE67354B1/en not_active IP Right Cessation
- 1991-01-16 FI FI910231A patent/FI101539B1/fi active
- 1991-01-18 NO NO910214A patent/NO179915C/no not_active IP Right Cessation
- 1991-01-18 PT PT96519A patent/PT96519B/pt not_active IP Right Cessation
- 1991-01-18 JP JP3019468A patent/JP2846484B2/ja not_active Expired - Lifetime
- 1991-01-18 HU HU91179A patent/HU208142B/hu unknown
- 1991-01-18 RU SU914894275A patent/RU2044740C1/ru active
- 1991-01-18 KR KR1019910000782A patent/KR0179368B1/ko not_active IP Right Cessation
- 1991-01-19 CN CN91100404A patent/CN1026791C/zh not_active Expired - Lifetime
-
1998
- 1998-09-28 KR KR1019980040259A patent/KR0179470B1/ko not_active IP Right Cessation
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Legal Events
Date | Code | Title | Description |
---|---|---|---|
FG2A | Definitive protection |
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