ES2915123R1 - Proceso para la síntesis de la sal sódica del ácido 4-[[(1R)-2-[5-(2-fluoro-3-metoxifenil)-3-[[2-fluoro-6-(trifluorometil)-fenil]metil]-3,6-dihidro-4-metil-2,6-dioxo-1(2H)-pirimidinil]-1-feniletil]amino]-butanoico (sal sódica de Elagolix) y productos intermedios de dicho proceso - Google Patents
Proceso para la síntesis de la sal sódica del ácido 4-[[(1R)-2-[5-(2-fluoro-3-metoxifenil)-3-[[2-fluoro-6-(trifluorometil)-fenil]metil]-3,6-dihidro-4-metil-2,6-dioxo-1(2H)-pirimidinil]-1-feniletil]amino]-butanoico (sal sódica de Elagolix) y productos intermedios de dicho procesoInfo
- Publication number
- ES2915123R1 ES2915123R1 ES202290012A ES202290012A ES2915123R1 ES 2915123 R1 ES2915123 R1 ES 2915123R1 ES 202290012 A ES202290012 A ES 202290012A ES 202290012 A ES202290012 A ES 202290012A ES 2915123 R1 ES2915123 R1 ES 2915123R1
- Authority
- ES
- Spain
- Prior art keywords
- fluoro
- sodium salt
- methyl
- dioxo
- phenylethyl
- 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
- 238000000034 method Methods 0.000 title 2
- 239000002253 acid Substances 0.000 title 1
- 230000015572 biosynthetic process Effects 0.000 title 1
- 239000013067 intermediate product Substances 0.000 title 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 title 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 title 1
- DQYGXRQUFSRDCH-UHFFFAOYSA-M sodium 4-[[2-[5-(2-fluoro-3-methoxyphenyl)-3-[[2-fluoro-6-(trifluoromethyl)phenyl]methyl]-4-methyl-2,6-dioxopyrimidin-1-yl]-1-phenylethyl]amino]butanoate Chemical compound [Na+].COc1cccc(c1F)-c1c(C)n(Cc2c(F)cccc2C(F)(F)F)c(=O)n(CC(NCCCC([O-])=O)c2ccccc2)c1=O DQYGXRQUFSRDCH-UHFFFAOYSA-M 0.000 title 1
- 159000000000 sodium salts Chemical class 0.000 title 1
- 238000003786 synthesis reaction Methods 0.000 title 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
- C07D239/52—Two oxygen atoms
- C07D239/54—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals
- C07D239/545—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals with other hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/553—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals with other hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms with halogen atoms or nitro radicals directly attached to ring carbon atoms, e.g. fluorouracil
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
- C07D239/52—Two oxygen atoms
- C07D239/54—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals
-
- A—HUMAN NECESSITIES
- A24—TOBACCO; CIGARS; CIGARETTES; SIMULATED SMOKING DEVICES; SMOKERS' REQUISITES
- A24C—MACHINES FOR MAKING CIGARS OR CIGARETTES
- A24C5/00—Making cigarettes; Making tipping materials for, or attaching filters or mouthpieces to, cigars or cigarettes
- A24C5/35—Adaptations of conveying apparatus for transporting cigarettes from making machine to packaging machine
- A24C5/352—Adaptations of conveying apparatus for transporting cigarettes from making machine to packaging machine using containers, i.e. boats
- A24C5/356—Emptying the boats into the hopper of the packaging machine
-
- A—HUMAN NECESSITIES
- A24—TOBACCO; CIGARS; CIGARETTES; SIMULATED SMOKING DEVICES; SMOKERS' REQUISITES
- A24C—MACHINES FOR MAKING CIGARS OR CIGARETTES
- A24C5/00—Making cigarettes; Making tipping materials for, or attaching filters or mouthpieces to, cigars or cigarettes
- A24C5/35—Adaptations of conveying apparatus for transporting cigarettes from making machine to packaging machine
- A24C5/352—Adaptations of conveying apparatus for transporting cigarettes from making machine to packaging machine using containers, i.e. boats
- A24C5/358—Boat constructions
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
-
- B—PERFORMING OPERATIONS; TRANSPORTING
- B65—CONVEYING; PACKING; STORING; HANDLING THIN OR FILAMENTARY MATERIAL
- B65B—MACHINES, APPARATUS OR DEVICES FOR, OR METHODS OF, PACKAGING ARTICLES OR MATERIALS; UNPACKING
- B65B19/00—Packaging rod-shaped or tubular articles susceptible to damage by abrasion or pressure, e.g. cigarettes, cigars, macaroni, spaghetti, drinking straws or welding electrodes
- B65B19/02—Packaging cigarettes
- B65B19/04—Arranging, feeding, or orientating the cigarettes
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| IT102019000015458A IT201900015458A1 (it) | 2019-09-03 | 2019-09-03 | Processo per la preparazione del sale sodico dell’acido 4-[[(1r)-2-[5-(2-fluoro-3-metossifenil)-3-[[2-fluoro-6-(trifluorometil)fenil]metil]-3,6-diidro-4-metil-2,6-diosso-1(2h)-pirimidinil]-1-feniletil]ammino]-butanoico (elagolix sale sodico) e intermedi di detto processo |
| IT102020000001390A IT202000001390A1 (it) | 2020-01-24 | 2020-01-24 | Processo per la preparazione del sale sodico dell’acido 4-[[(1r)-2-[5-(2-fluoro-3-metossifenil)-3-[[2-fluoro-6-(trifluorometil)fenil]metil]-3,6-diidro-4-metil-2,6-diosso-1(2h)-pirimidinil]-1-feniletil]ammino]-butanoico (elagolix sale sodico) e intermedi di detto processo |
| PCT/IB2020/057065 WO2021044230A1 (en) | 2019-09-03 | 2020-07-27 | Process for the synthesis of the sodium salt of 4-[[(lr)-2-[5-(2-fluoro-3-methoxyphenyl)-3-[[2-fluoro-6-(trifluoromethyl)-phenyl]methyl]-3,6-dihydro-4-methyl-2,6-dioxo-l(2h)-pyrimidinyl]-l- phenylethyl]amino]-butanoic acid (elagolix sodium salt) and intermediates of said process |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| ES2915123A2 ES2915123A2 (es) | 2022-06-20 |
| ES2915123R1 true ES2915123R1 (es) | 2023-07-14 |
| ES2915123B2 ES2915123B2 (es) | 2024-04-24 |
Family
ID=72234870
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES202290012A Active ES2915123B2 (es) | 2019-09-03 | 2020-07-27 | Proceso para la síntesis de la sal sódica del ácido 4-[[(1R)-2-[5-(2-fluoro-3-metoxifenil)-3-[[2-fluoro-6-(trifluorometil)-fenil]metil]-3,6-dihidro-4-metil-2,6-dioxo-1(2H)-pirimidinil]-1-feniletil]amino]-butanoico (sal sódica de Elagolix) y productos intermedios de dicho proceso |
Country Status (10)
| Country | Link |
|---|---|
| US (1) | US11840519B2 (es) |
| CN (1) | CN114641468B (es) |
| BR (1) | BR112022003622A2 (es) |
| CA (1) | CA3149179A1 (es) |
| CH (1) | CH718005B1 (es) |
| DE (1) | DE112020004177B4 (es) |
| ES (1) | ES2915123B2 (es) |
| FR (1) | FR3100246B1 (es) |
| GB (1) | GB2603328B (es) |
| WO (1) | WO2021044230A1 (es) |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BR112021000973A2 (pt) | 2018-07-23 | 2021-04-20 | Abbvie Inc. | composições e processos de sódio de elagolix |
Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2005007165A1 (en) * | 2003-07-07 | 2005-01-27 | Neurocrine Biosciences, Inc. | Pyrimidine-2, 4-dione derivatives as gonadotropin-releasing hormone receptor antagonists |
| WO2017221144A1 (en) * | 2016-06-20 | 2017-12-28 | Dr. Reddy's Laboratories Limited | Process for the preparation of elagolix sodium and its polymorph |
| WO2018198086A1 (en) * | 2017-04-28 | 2018-11-01 | Lupin Limited | Process for the preparation of elagolix and pharmaceutically acceptable salts thereof |
| WO2019115019A1 (en) * | 2017-12-11 | 2019-06-20 | Synthon B.V. | Process for preparing elagolix |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2005113516A1 (en) | 2004-05-14 | 2005-12-01 | Neurocrine Biosciences, Inc. | Uracil-type gonadotropin-releasing hormone receptor antagonists and methods related thereto |
| CN109293634A (zh) | 2018-12-04 | 2019-02-01 | 中国药科大学 | 恶拉戈利杂质的制备方法 |
| CN109651265A (zh) * | 2019-02-16 | 2019-04-19 | 安徽诺全药业有限公司 | 一种Elagolix的制备方法 |
-
2020
- 2020-07-27 DE DE112020004177.8T patent/DE112020004177B4/de active Active
- 2020-07-27 CA CA3149179A patent/CA3149179A1/en active Pending
- 2020-07-27 FR FR2007887A patent/FR3100246B1/fr active Active
- 2020-07-27 BR BR112022003622A patent/BR112022003622A2/pt unknown
- 2020-07-27 US US17/639,638 patent/US11840519B2/en active Active
- 2020-07-27 CH CH000210/2022A patent/CH718005B1/it unknown
- 2020-07-27 WO PCT/IB2020/057065 patent/WO2021044230A1/en active Application Filing
- 2020-07-27 ES ES202290012A patent/ES2915123B2/es active Active
- 2020-07-27 GB GB2203781.6A patent/GB2603328B/en active Active
- 2020-07-27 CN CN202080062002.7A patent/CN114641468B/zh active Active
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2005007165A1 (en) * | 2003-07-07 | 2005-01-27 | Neurocrine Biosciences, Inc. | Pyrimidine-2, 4-dione derivatives as gonadotropin-releasing hormone receptor antagonists |
| WO2017221144A1 (en) * | 2016-06-20 | 2017-12-28 | Dr. Reddy's Laboratories Limited | Process for the preparation of elagolix sodium and its polymorph |
| WO2018198086A1 (en) * | 2017-04-28 | 2018-11-01 | Lupin Limited | Process for the preparation of elagolix and pharmaceutically acceptable salts thereof |
| WO2019115019A1 (en) * | 2017-12-11 | 2019-06-20 | Synthon B.V. | Process for preparing elagolix |
Also Published As
| Publication number | Publication date |
|---|---|
| GB202203781D0 (en) | 2022-05-04 |
| WO2021044230A8 (en) | 2022-04-07 |
| DE112020004177T5 (de) | 2022-06-30 |
| GB2603328B (en) | 2024-02-07 |
| GB2603328A (en) | 2022-08-03 |
| WO2021044230A1 (en) | 2021-03-11 |
| ES2915123B2 (es) | 2024-04-24 |
| CA3149179A1 (en) | 2021-03-11 |
| FR3100246B1 (fr) | 2024-03-08 |
| BR112022003622A2 (pt) | 2022-05-24 |
| US11840519B2 (en) | 2023-12-12 |
| DE112020004177B4 (de) | 2024-10-02 |
| CN114641468A (zh) | 2022-06-17 |
| CH718005B1 (it) | 2023-07-31 |
| US20220281829A1 (en) | 2022-09-08 |
| FR3100246A1 (fr) | 2021-03-05 |
| CN114641468B (zh) | 2024-11-12 |
| ES2915123A2 (es) | 2022-06-20 |
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