IN2013MU03696A - - Google Patents
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- Publication number
- IN2013MU03696A IN2013MU03696A IN3696MU2013A IN2013MU03696A IN 2013MU03696 A IN2013MU03696 A IN 2013MU03696A IN 3696MU2013 A IN3696MU2013 A IN 3696MU2013A IN 2013MU03696 A IN2013MU03696 A IN 2013MU03696A
- Authority
- IN
- India
- Prior art keywords
- iii
- diethyl
- acetamido
- malonate
- fingolimod hydrochloride
- Prior art date
Links
- SWZTYAVBMYWFGS-UHFFFAOYSA-N fingolimod hydrochloride Chemical compound Cl.CCCCCCCCC1=CC=C(CCC(N)(CO)CO)C=C1 SWZTYAVBMYWFGS-UHFFFAOYSA-N 0.000 abstract 3
- YURZVKRFVMTWMC-UHFFFAOYSA-N 1-(2-iodoethyl)-4-octylbenzene Chemical compound CCCCCCCCC1=CC=C(CCI)C=C1 YURZVKRFVMTWMC-UHFFFAOYSA-N 0.000 abstract 2
- 229960004967 fingolimod hydrochloride Drugs 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 1
- ISOLMABRZPQKOV-UHFFFAOYSA-N diethyl 2-acetamidopropanedioate Chemical compound CCOC(=O)C(NC(C)=O)C(=O)OCC ISOLMABRZPQKOV-UHFFFAOYSA-N 0.000 abstract 1
- 125000004177 diethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 abstract 1
- UKFXDFUAPNAMPJ-UHFFFAOYSA-N ethylmalonic acid Chemical compound CCC(C(O)=O)C(O)=O UKFXDFUAPNAMPJ-UHFFFAOYSA-N 0.000 abstract 1
- 239000012535 impurity Substances 0.000 abstract 1
- 239000012336 iodinating agent Substances 0.000 abstract 1
- 238000000034 method Methods 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
- 230000001105 regulatory effect Effects 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C213/00—Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton
- C07C213/02—Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton by reactions involving the formation of amino groups from compounds containing hydroxy groups or etherified or esterified hydroxy groups
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C213/00—Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C215/00—Compounds containing amino and hydroxy groups bound to the same carbon skeleton
- C07C215/02—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton
- C07C215/22—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being unsaturated
- C07C215/28—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being unsaturated and containing six-membered aromatic rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C231/00—Preparation of carboxylic acid amides
- C07C231/12—Preparation of carboxylic acid amides by reactions not involving the formation of carboxamide groups
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/07—Optical isomers
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
A process for preparation of diethyl 2-acetamido-2-(4-octyI phenyl)ethyl malonate (III), a key intermediate of fingolimod hydrochloride comprising reaction of 2-(4-octylphenyl)ethyl iodide (IV) with diethyl acetamido malonate in presence of a base and an iodinating agent and in an organic solvent. The compound of formula (III) thus obtained provided fingolimod hydrochloride (la) is having associated impurities below the regulatory limits.
Priority Applications (6)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US15/035,306 US9643914B2 (en) | 2013-11-25 | 2014-11-14 | Fingolimod hydrochloride process |
| IN3696MU2013 IN2013MU03696A (en) | 2013-11-25 | 2014-11-14 | |
| ES14853182T ES2729404T3 (en) | 2013-11-25 | 2014-11-14 | Fingolimod hydrochloride process |
| CA2930089A CA2930089C (en) | 2013-11-25 | 2014-11-14 | Fingolimod hydrochloride process |
| PCT/IN2014/000720 WO2015092809A2 (en) | 2013-11-25 | 2014-11-14 | Fingolimod hydrochloride process |
| EP14853182.5A EP3074374B1 (en) | 2013-11-25 | 2014-11-14 | Fingolimod hydrochloride process |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| IN3696MU2013 IN2013MU03696A (en) | 2013-11-25 | 2014-11-14 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| IN2013MU03696A true IN2013MU03696A (en) | 2015-07-31 |
Family
ID=52823744
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| IN3696MU2013 IN2013MU03696A (en) | 2013-11-25 | 2014-11-14 |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US9643914B2 (en) |
| EP (1) | EP3074374B1 (en) |
| CA (1) | CA2930089C (en) |
| ES (1) | ES2729404T3 (en) |
| IN (1) | IN2013MU03696A (en) |
| WO (1) | WO2015092809A2 (en) |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2020165672A1 (en) | 2019-02-15 | 2020-08-20 | Shivalik Rasayan Limited | Process for preparation of highly pure fingolimod hydrochloride |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE69321823T2 (en) | 1992-10-21 | 1999-06-02 | Taito Co., Ltd., Tokio/Tokyo | 2-AMINO-1, 3-PROPANEDIOL COMPOUND AND IMMUNOSUPPRESSIUM |
| DK1129066T3 (en) | 1998-11-11 | 2005-03-29 | Novartis Ag | Preparation of 2-amino-2- [2- (C2-20 alkylphenyl) ethyl] propane-1,3-diols |
| US6423871B1 (en) * | 1999-02-26 | 2002-07-23 | University Of South Florida | Efficient synthesis of secondary amines by selective alkylation of primary amines |
| WO2012070059A1 (en) * | 2010-11-25 | 2012-05-31 | Shilpa Medicare Limited | Fingolimod polymorphs and their processes |
| US9216943B2 (en) | 2011-04-29 | 2015-12-22 | Dr. Reddy's Laboratories Ltd. | Preparation of fingolimod and its salts |
| WO2013111162A2 (en) | 2012-01-25 | 2013-08-01 | Glenmark Generics Limited | Process for preparation of fingolimod |
-
2014
- 2014-11-14 ES ES14853182T patent/ES2729404T3/en active Active
- 2014-11-14 IN IN3696MU2013 patent/IN2013MU03696A/en unknown
- 2014-11-14 EP EP14853182.5A patent/EP3074374B1/en active Active
- 2014-11-14 US US15/035,306 patent/US9643914B2/en active Active
- 2014-11-14 WO PCT/IN2014/000720 patent/WO2015092809A2/en not_active Ceased
- 2014-11-14 CA CA2930089A patent/CA2930089C/en active Active
Also Published As
| Publication number | Publication date |
|---|---|
| EP3074374A2 (en) | 2016-10-05 |
| ES2729404T3 (en) | 2019-11-04 |
| CA2930089A1 (en) | 2015-06-25 |
| WO2015092809A3 (en) | 2015-08-13 |
| US20160289166A1 (en) | 2016-10-06 |
| WO2015092809A2 (en) | 2015-06-25 |
| CA2930089C (en) | 2021-08-03 |
| EP3074374B1 (en) | 2019-03-13 |
| US9643914B2 (en) | 2017-05-09 |
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