ES2176036T3 - Sintesis quimica de derivados de morfolina. - Google Patents
Sintesis quimica de derivados de morfolina.Info
- Publication number
- ES2176036T3 ES2176036T3 ES99957055T ES99957055T ES2176036T3 ES 2176036 T3 ES2176036 T3 ES 2176036T3 ES 99957055 T ES99957055 T ES 99957055T ES 99957055 T ES99957055 T ES 99957055T ES 2176036 T3 ES2176036 T3 ES 2176036T3
- Authority
- ES
- Spain
- Prior art keywords
- alkyl
- group
- formula
- compound
- iodine
- 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
- YNAVUWVOSKDBBP-UHFFFAOYSA-N Morpholine Chemical class C1COCCN1 YNAVUWVOSKDBBP-UHFFFAOYSA-N 0.000 title 1
- 238000003786 synthesis reaction Methods 0.000 title 1
- 150000002431 hydrogen Chemical class 0.000 abstract 6
- 150000001875 compounds Chemical class 0.000 abstract 4
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 3
- WKBOTKDWSSQWDR-UHFFFAOYSA-N Bromine atom Chemical compound [Br] WKBOTKDWSSQWDR-UHFFFAOYSA-N 0.000 abstract 3
- GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Substances BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 abstract 3
- 229910052794 bromium Inorganic materials 0.000 abstract 3
- 229910052739 hydrogen Inorganic materials 0.000 abstract 3
- 239000001257 hydrogen Substances 0.000 abstract 3
- 125000001309 chloro group Chemical group Cl* 0.000 abstract 2
- 125000001153 fluoro group Chemical group F* 0.000 abstract 2
- PNDPGZBMCMUPRI-UHFFFAOYSA-N iodine Chemical compound II PNDPGZBMCMUPRI-UHFFFAOYSA-N 0.000 abstract 2
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 1
- ZCYVEMRRCGMTRW-UHFFFAOYSA-N 7553-56-2 Chemical compound [I] ZCYVEMRRCGMTRW-UHFFFAOYSA-N 0.000 abstract 1
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 abstract 1
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 abstract 1
- AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical compound CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 125000005228 aryl sulfonate group Chemical group 0.000 abstract 1
- 229910052801 chlorine Inorganic materials 0.000 abstract 1
- 239000000460 chlorine Substances 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 150000002367 halogens Chemical class 0.000 abstract 1
- 229910052740 iodine Inorganic materials 0.000 abstract 1
- 239000011630 iodine Substances 0.000 abstract 1
- 239000003960 organic solvent Substances 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- JOXIMZWYDAKGHI-UHFFFAOYSA-N toluene-4-sulfonic acid Chemical compound CC1=CC=C(S(O)(=O)=O)C=C1 JOXIMZWYDAKGHI-UHFFFAOYSA-N 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
- C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Neurology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Biomedical Technology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Neurosurgery (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Psychiatry (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
Un procedimiento para la preparación de un compuesto de fórmula en la que R2 y R3 se seleccionan independientemente del grupo constituido por (1) hidrógeno (2) alquilo C1-6, (3) alquenilo C2-6, y (4) fenilo; R6, R7 y R8 se seleccionan independientemente del grupo constituido por (1) hidrógeno (2) alquilo C1-6, (3) fluoro, (4) cloro, (5) bromo, (6) yodo, y (7) CF3 R11, R12 y R13 se seleccionan independientemente del grupo constituido por (1) hidrógeno (2) alquilo C1-6, (3) fluoro, (4) cloro, (5) bromo, (6) yodo, y (7) CF3, y Z es alquilo C1-4, que comprende: (i) hacer reaccionar un compuesto de fórmula o una sal del mismo, en la que R2, R3, R6, R7, R8, R11, R12, R13 y Z son como se definieron previamente, con un compuesto de fórmula en la que LG es un grupo saliente seleccionado entre halógeno (por ejemplo bromo, cloro o yodo) o un grupo alquilo o arilsulfonato (por ejemplo mesilato o tosilato) en un disolvente orgánico y en presencia de una base; y (ii) recoger el compuesto cristalino resultante de fórmula.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB9813025.5A GB9813025D0 (en) | 1998-06-16 | 1998-06-16 | Chemical synthesis |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ES2176036T3 true ES2176036T3 (es) | 2002-11-16 |
Family
ID=10833892
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES99957055T Expired - Lifetime ES2176036T3 (es) | 1998-06-16 | 1999-06-10 | Sintesis quimica de derivados de morfolina. |
Country Status (28)
| Country | Link |
|---|---|
| US (2) | US6297376B1 (es) |
| EP (1) | EP1087966B1 (es) |
| JP (2) | JP4647783B2 (es) |
| KR (1) | KR100619589B1 (es) |
| CN (1) | CN1131864C (es) |
| AR (1) | AR018877A1 (es) |
| AT (1) | ATE217308T1 (es) |
| AU (1) | AU746721B2 (es) |
| BR (1) | BR9911250A (es) |
| CA (1) | CA2334821C (es) |
| CZ (1) | CZ299257B6 (es) |
| DE (1) | DE69901444T2 (es) |
| DK (1) | DK1087966T3 (es) |
| EA (1) | EA003468B1 (es) |
| ES (1) | ES2176036T3 (es) |
| GB (1) | GB9813025D0 (es) |
| HR (1) | HRP20000878B1 (es) |
| HU (1) | HUP0102867A3 (es) |
| IL (2) | IL139946A0 (es) |
| NZ (1) | NZ508558A (es) |
| PL (1) | PL196778B1 (es) |
| PT (1) | PT1087966E (es) |
| SI (1) | SI1087966T1 (es) |
| SK (1) | SK283380B6 (es) |
| TW (1) | TW526199B (es) |
| UA (1) | UA66866C2 (es) |
| WO (1) | WO1999065900A1 (es) |
| YU (1) | YU76500A (es) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AR030284A1 (es) | 2000-06-08 | 2003-08-20 | Merck & Co Inc | Proceso para la sintesis de (2r, 2-alfa-r,3a) -2-[1-(3,5-bis(trifluorometil) fenil) etoxi]-3-(4-fluorofenil)-1,4-oxazina; dicho compuesto y sus formas polimorficas |
| GB0014876D0 (en) * | 2000-06-16 | 2000-08-09 | Merck Sharp & Dohme | Chemical synthesis |
| UA76810C2 (uk) | 2001-12-10 | 2006-09-15 | Мерк Енд Ко., Інк. | Фармацевтична композиція антагоніста рецептора тахікініну у формі наночастинок |
| AR039625A1 (es) | 2002-04-18 | 2005-03-02 | Merck & Co Inc | Proceso para la preparacion de 5-((2(r)--(1(r)- (3,5-bis (trifluormetil) fenil)etoxi-3 (s) - (4-fluorfenil) -4-morfolinil) metil) -1,2-dihidro-3h-1,2,4-triazol-3-ona |
| AU2003259866A1 (en) | 2002-08-21 | 2004-03-11 | Merck And Co., Inc. | Process for preparing 3-chloromethyl-1,2,4-triazolin-5-one |
| EP1984359A1 (en) * | 2006-02-03 | 2008-10-29 | Glenmark Pharmaceuticals Limited | Amorphous and crystalline forms of aprepitant and processes for the preparation thereof |
| WO2012146692A1 (en) | 2011-04-29 | 2012-11-01 | Sandoz Ag | Novel intermediates for the preparation of highly pure aprepitant or fosaprepitant |
| ITMI20130273A1 (it) * | 2013-02-26 | 2014-08-27 | Olon Spa | Procedimento per la preparazione di aprepitant |
| CN103288813A (zh) * | 2013-06-04 | 2013-09-11 | 四川百利药业有限责任公司 | 一种阿瑞匹坦的制备方法 |
| CN104628663A (zh) * | 2013-11-08 | 2015-05-20 | 中山奕安泰医药科技有限公司 | 3-氯甲基-1,2,4-三唑啉-5-酮的合成方法 |
| CN107698574B (zh) * | 2017-11-23 | 2020-12-01 | 中山奕安泰医药科技有限公司 | 一种高纯度阿瑞匹坦的精制制备工艺 |
| CN109485613B (zh) * | 2018-11-21 | 2022-05-13 | 江苏慧聚药业股份有限公司 | 阿瑞匹坦和福沙匹坦边链片段的制备方法 |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IL111960A (en) * | 1993-12-17 | 1999-12-22 | Merck & Co Inc | Morpholines and thiomorpholines their preparation and pharmaceutical compositions containing them |
| SG52217A1 (en) * | 1993-12-29 | 1998-09-28 | Merck Sharp & Dohme | Substituted morpholine derivatives and their use as therapeutic agents |
| IL112778A0 (en) * | 1994-03-04 | 1995-05-26 | Merck & Co Inc | Substituted heterocycles, their preparation and pharmaceutical compositions containing them |
| EP0758329A1 (en) * | 1994-05-05 | 1997-02-19 | MERCK SHARP & DOHME LTD. | Morpholine derivatives and their use as antagonists of tachikinins |
-
1998
- 1998-06-16 GB GBGB9813025.5A patent/GB9813025D0/en not_active Ceased
-
1999
- 1999-06-10 SI SI9930053T patent/SI1087966T1/xx unknown
- 1999-06-10 EP EP99957055A patent/EP1087966B1/en not_active Expired - Lifetime
- 1999-06-10 WO PCT/GB1999/001842 patent/WO1999065900A1/en active IP Right Grant
- 1999-06-10 US US09/719,712 patent/US6297376B1/en not_active Expired - Lifetime
- 1999-06-10 YU YU76500A patent/YU76500A/sh unknown
- 1999-06-10 NZ NZ508558A patent/NZ508558A/en not_active IP Right Cessation
- 1999-06-10 JP JP2000554725A patent/JP4647783B2/ja not_active Expired - Fee Related
- 1999-06-10 CN CN998074667A patent/CN1131864C/zh not_active Expired - Fee Related
- 1999-06-10 DK DK99957055T patent/DK1087966T3/da active
- 1999-06-10 CA CA002334821A patent/CA2334821C/en not_active Expired - Fee Related
- 1999-06-10 BR BR9911250-7A patent/BR9911250A/pt not_active Application Discontinuation
- 1999-06-10 CZ CZ20004734A patent/CZ299257B6/cs not_active IP Right Cessation
- 1999-06-10 DE DE69901444T patent/DE69901444T2/de not_active Expired - Lifetime
- 1999-06-10 AT AT99957055T patent/ATE217308T1/de active
- 1999-06-10 IL IL13994699A patent/IL139946A0/xx active IP Right Grant
- 1999-06-10 KR KR1020007014230A patent/KR100619589B1/ko not_active IP Right Cessation
- 1999-06-10 UA UA2001010329A patent/UA66866C2/uk unknown
- 1999-06-10 EA EA200100040A patent/EA003468B1/ru not_active IP Right Cessation
- 1999-06-10 PL PL344581A patent/PL196778B1/pl unknown
- 1999-06-10 SK SK1921-2000A patent/SK283380B6/sk not_active IP Right Cessation
- 1999-06-10 PT PT99957055T patent/PT1087966E/pt unknown
- 1999-06-10 AU AU42813/99A patent/AU746721B2/en not_active Ceased
- 1999-06-10 HU HU0102867A patent/HUP0102867A3/hu unknown
- 1999-06-10 ES ES99957055T patent/ES2176036T3/es not_active Expired - Lifetime
- 1999-06-16 AR ARP990102885A patent/AR018877A1/es active IP Right Grant
- 1999-06-25 TW TW088110746A patent/TW526199B/zh not_active IP Right Cessation
-
2000
- 2000-11-28 IL IL139946A patent/IL139946A/en not_active IP Right Cessation
- 2000-12-15 HR HR20000878A patent/HRP20000878B1/xx not_active IP Right Cessation
-
2001
- 2001-09-10 US US09/950,286 patent/US6407255B2/en not_active Expired - Lifetime
-
2010
- 2010-04-14 JP JP2010092803A patent/JP5285652B2/ja not_active Expired - Fee Related
Also Published As
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FG2A | Definitive protection |
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