IN2014DN09774A - - Google Patents
Info
- Publication number
- IN2014DN09774A IN2014DN09774A IN9774DEN2014A IN2014DN09774A IN 2014DN09774 A IN2014DN09774 A IN 2014DN09774A IN 9774DEN2014 A IN9774DEN2014 A IN 9774DEN2014A IN 2014DN09774 A IN2014DN09774 A IN 2014DN09774A
- Authority
- IN
- India
- Prior art keywords
- synthesis
- activated
- improved
- disclosed embodiments
- intermediates
- Prior art date
Links
- 238000003786 synthesis reaction Methods 0.000 abstract 4
- 230000015572 biosynthetic process Effects 0.000 abstract 3
- VZCYOOQTPOCHFL-OWOJBTEDSA-N Fumaric acid Chemical class OC(=O)\C=C\C(O)=O VZCYOOQTPOCHFL-OWOJBTEDSA-N 0.000 abstract 2
- 239000000543 intermediate Substances 0.000 abstract 2
- JVSFQJZRHXAUGT-UHFFFAOYSA-N 2,2-dimethylpropanoyl chloride Chemical compound CC(C)(C)C(Cl)=O JVSFQJZRHXAUGT-UHFFFAOYSA-N 0.000 abstract 1
- BTJIUGUIPKRLHP-UHFFFAOYSA-N 4-nitrophenol Chemical compound OC1=CC=C([N+]([O-])=O)C=C1 BTJIUGUIPKRLHP-UHFFFAOYSA-N 0.000 abstract 1
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 abstract 1
- 230000003213 activating effect Effects 0.000 abstract 1
- 125000004103 aminoalkyl group Chemical group 0.000 abstract 1
- 150000001540 azides Chemical class 0.000 abstract 1
- 229910052801 chlorine Inorganic materials 0.000 abstract 1
- 239000000460 chlorine Substances 0.000 abstract 1
- WRJWRGBVPUUDLA-UHFFFAOYSA-N chlorosulfonyl isocyanate Chemical compound ClS(=O)(=O)N=C=O WRJWRGBVPUUDLA-UHFFFAOYSA-N 0.000 abstract 1
- 150000002148 esters Chemical class 0.000 abstract 1
- YYLWXDIGYFPUSK-ONEGZZNKSA-N ethyl (e)-4-chloro-4-oxobut-2-enoate Chemical compound CCOC(=O)\C=C\C(Cl)=O YYLWXDIGYFPUSK-ONEGZZNKSA-N 0.000 abstract 1
- -1 for example Chemical compound 0.000 abstract 1
- 238000011065 in-situ storage Methods 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 125000000636 p-nitrophenyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1*)[N+]([O-])=O 0.000 abstract 1
- 125000004044 trifluoroacetyl group Chemical group FC(C(=O)*)(F)F 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
- C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
- C07D241/06—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having one or two double bonds between ring members or between ring members and non-ring members
- C07D241/08—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having one or two double bonds between ring members or between ring members and non-ring members with oxygen atoms directly attached to ring carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C201/00—Preparation of esters of nitric or nitrous acid or of compounds containing nitro or nitroso groups bound to a carbon skeleton
- C07C201/06—Preparation of nitro compounds
- C07C201/12—Preparation of nitro compounds by reactions not involving the formation of nitro groups
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C67/00—Preparation of carboxylic acid esters
- C07C67/30—Preparation of carboxylic acid esters by modifying the acid moiety of the ester, such modification not being an introduction of an ester group
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C67/00—Preparation of carboxylic acid esters
- C07C67/39—Preparation of carboxylic acid esters by oxidation of groups which are precursors for the acid moiety of the ester
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Plural Heterocyclic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Disclosed embodiments relate to improved methods for the synthesis of activated fumarate intermediates and their use in chemical synthesis. Disclosed embodiments describe the synthesis of activated fumarate esters including those derived from activating groups including: 4- nitrophenyl, diphenylphophoryl azide , pivaloyl chloride, chlorosulfonyl isocyanate , p- nitrophenol , MEF , trifluoroacetyl and chlorine , for example , ethyl fumaroyl chloride and the subsequent use of the activated ester in situ. Further embodiments describe the improved synthesis of substituted aminoalkyl -diketopiperazines from unisolated and unpurified intermediates allowing for improved yields and reactor throughput.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261639536P | 2012-04-27 | 2012-04-27 | |
| PCT/US2013/032162 WO2013162764A1 (en) | 2012-04-27 | 2013-03-15 | Methods for the synthesis of ethylfumarates and their use as intermediates |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| IN2014DN09774A true IN2014DN09774A (en) | 2015-07-31 |
Family
ID=49477848
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| IN9774DEN2014 IN2014DN09774A (en) | 2012-04-27 | 2013-03-15 |
Country Status (16)
| Country | Link |
|---|---|
| US (6) | US9193691B2 (en) |
| EP (1) | EP2841422B1 (en) |
| JP (1) | JP6241682B2 (en) |
| KR (1) | KR20150023315A (en) |
| CN (2) | CN107879938A (en) |
| AU (2) | AU2013252901B2 (en) |
| BR (1) | BR112014026809A2 (en) |
| CA (1) | CA2871126C (en) |
| HK (1) | HK1207382A1 (en) |
| IL (1) | IL235247A0 (en) |
| IN (1) | IN2014DN09774A (en) |
| MX (1) | MX361470B (en) |
| RU (1) | RU2014143116A (en) |
| SG (1) | SG11201406970QA (en) |
| WO (1) | WO2013162764A1 (en) |
| ZA (1) | ZA201408429B (en) |
Families Citing this family (27)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9006175B2 (en) | 1999-06-29 | 2015-04-14 | Mannkind Corporation | Potentiation of glucose elimination |
| ES2425392T3 (en) | 2002-03-20 | 2013-10-15 | Mannkind Corporation | Cartridge for an inhalation device |
| JP5078014B2 (en) | 2004-08-20 | 2012-11-21 | マンカインド コーポレイション | Catalytic reaction of diketopiperazine synthesis. |
| PL2322180T3 (en) | 2004-08-23 | 2015-10-30 | Mannkind Corp | Diketopiperazine salts for drug delivery |
| CN104324366B (en) | 2005-09-14 | 2016-10-05 | 曼金德公司 | Method for preparation of drug based on improving the active agent affinity to crystalline microparticle surfaces |
| KR20080096809A (en) | 2006-02-22 | 2008-11-03 | 맨카인드 코포레이션 | Method for Improving Pharmaceutical Properties of Microparticles Containing Diketopiperazine and Active Agents |
| US8485180B2 (en) | 2008-06-13 | 2013-07-16 | Mannkind Corporation | Dry powder drug delivery system |
| MY155524A (en) | 2008-06-13 | 2015-10-30 | Mannkind Corp | A dry powder inhaler and system for drug delivery |
| KR101628410B1 (en) | 2008-06-20 | 2016-06-08 | 맨카인드 코포레이션 | An interactive apparatus and method for real-time profiling of inhalation efforts |
| TWI532497B (en) | 2008-08-11 | 2016-05-11 | 曼凱公司 | Ultra-fast use of insulin |
| US8314106B2 (en) | 2008-12-29 | 2012-11-20 | Mannkind Corporation | Substituted diketopiperazine analogs for use as drug delivery agents |
| DK2405963T3 (en) | 2009-03-11 | 2013-12-16 | Mannkind Corp | DEVICE, SYSTEM AND PROCEDURE FOR MEASURING RESISTANCE IN AN INHALATOR |
| KR20180079458A (en) | 2009-06-12 | 2018-07-10 | 맨카인드 코포레이션 | Diketopiperazine microparticles with defined specific surface areas |
| US9016147B2 (en) | 2009-11-03 | 2015-04-28 | Mannkind Corporation | Apparatus and method for simulating inhalation efforts |
| BR112012033060A2 (en) | 2010-06-21 | 2018-02-27 | Mannkind Corp | Dry powder drug release system methods |
| AU2012236150B2 (en) | 2011-04-01 | 2016-03-31 | Mannkind Corporation | Blister package for pharmaceutical cartridges |
| WO2012174472A1 (en) | 2011-06-17 | 2012-12-20 | Mannkind Corporation | High capacity diketopiperazine microparticles |
| AU2012328885B2 (en) | 2011-10-24 | 2017-08-31 | Mannkind Corporation | Methods and compositions for treating pain |
| BR112014026809A2 (en) * | 2012-04-27 | 2017-06-27 | Mannkind Corp | methods for the synthesis of activated ethyl fumarates and their use as intermediates |
| SG10201605800UA (en) | 2012-07-12 | 2016-09-29 | Mannkind Corp | Dry powder drug delivery system and methods |
| US10159644B2 (en) | 2012-10-26 | 2018-12-25 | Mannkind Corporation | Inhalable vaccine compositions and methods |
| AU2014228415B2 (en) | 2013-03-15 | 2018-08-09 | Mannkind Corporation | Microcrystalline diketopiperazine compositions and methods |
| KR102465025B1 (en) | 2013-07-18 | 2022-11-09 | 맨카인드 코포레이션 | Heat-stable dry powder pharmaceutical compositions and methods |
| WO2015021064A1 (en) | 2013-08-05 | 2015-02-12 | Mannkind Corporation | Insufflation apparatus and methods |
| US10307464B2 (en) | 2014-03-28 | 2019-06-04 | Mannkind Corporation | Use of ultrarapid acting insulin |
| US10561806B2 (en) | 2014-10-02 | 2020-02-18 | Mannkind Corporation | Mouthpiece cover for an inhaler |
| CN117646042B (en) * | 2023-11-13 | 2025-04-11 | 浙江工业大学 | A kind of preparation method of fumaric acid monoester |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3407203A (en) | 1965-03-22 | 1968-10-22 | Union Carbide Corp | Novel process for the preparation of diketopiperazines |
| US5352461A (en) * | 1992-03-11 | 1994-10-04 | Pharmaceutical Discovery Corporation | Self assembling diketopiperazine drug delivery system |
| DE10019879A1 (en) | 2000-04-20 | 2001-10-25 | Degussa | Production of known and new 2,5-diketopiperazine derivatives useful for the synthesis of bioactive compounds, e.g. cyclo(Lys-Lys) |
| JP5078014B2 (en) | 2004-08-20 | 2012-11-21 | マンカインド コーポレイション | Catalytic reaction of diketopiperazine synthesis. |
| PL2322180T3 (en) | 2004-08-23 | 2015-10-30 | Mannkind Corp | Diketopiperazine salts for drug delivery |
| KR20080096809A (en) * | 2006-02-22 | 2008-11-03 | 맨카인드 코포레이션 | Method for Improving Pharmaceutical Properties of Microparticles Containing Diketopiperazine and Active Agents |
| JP5788806B2 (en) * | 2008-12-29 | 2015-10-07 | マンカインド コーポレイション | Substituted diketopiperazines and salts thereof for drug delivery agents, therapeutic compositions containing them, fine particle compositions and dry powder compositions, and methods for preparing the same |
| US8314106B2 (en) | 2008-12-29 | 2012-11-20 | Mannkind Corporation | Substituted diketopiperazine analogs for use as drug delivery agents |
| EP2427430B1 (en) * | 2009-05-04 | 2014-09-10 | The Royal Institution for the Advancement of Learning/McGill University | 5-oxo-ete receptor antagonist compounds |
| CN101851213A (en) * | 2010-06-21 | 2010-10-06 | 于清 | Synthetic methods of 3,6-bis(4-bisfumaroyl aminobutyl)-2,5-diketopiperazine and salt substitute thereof |
| CN103534242B (en) | 2011-02-10 | 2016-04-20 | 曼坎德公司 | Formation of N-protected bis-3,6-(4-aminoalkyl)-2,5-diketopiperazines |
| BR112014026809A2 (en) * | 2012-04-27 | 2017-06-27 | Mannkind Corp | methods for the synthesis of activated ethyl fumarates and their use as intermediates |
-
2013
- 2013-03-15 BR BR112014026809A patent/BR112014026809A2/en not_active Application Discontinuation
- 2013-03-15 CA CA2871126A patent/CA2871126C/en active Active
- 2013-03-15 JP JP2015508969A patent/JP6241682B2/en active Active
- 2013-03-15 HK HK15108108.5A patent/HK1207382A1/en unknown
- 2013-03-15 EP EP13781305.1A patent/EP2841422B1/en active Active
- 2013-03-15 AU AU2013252901A patent/AU2013252901B2/en active Active
- 2013-03-15 KR KR20147033484A patent/KR20150023315A/en not_active Withdrawn
- 2013-03-15 IN IN9774DEN2014 patent/IN2014DN09774A/en unknown
- 2013-03-15 CN CN201711143342.9A patent/CN107879938A/en active Pending
- 2013-03-15 WO PCT/US2013/032162 patent/WO2013162764A1/en active Application Filing
- 2013-03-15 RU RU2014143116A patent/RU2014143116A/en not_active Application Discontinuation
- 2013-03-15 MX MX2014013075A patent/MX361470B/en active IP Right Grant
- 2013-03-15 CN CN201380033409.7A patent/CN104797563B/en active Active
- 2013-03-15 SG SG11201406970QA patent/SG11201406970QA/en unknown
- 2013-03-15 US US13/834,106 patent/US9193691B2/en active Active
-
2014
- 2014-10-21 IL IL235247A patent/IL235247A0/en unknown
- 2014-11-17 ZA ZA2014/08429A patent/ZA201408429B/en unknown
-
2015
- 2015-11-23 US US14/949,489 patent/US10071969B2/en active Active
-
2018
- 2018-02-27 AU AU2018201397A patent/AU2018201397B2/en active Active
- 2018-09-10 US US16/126,323 patent/US10858325B2/en active Active
-
2020
- 2020-12-07 US US17/113,540 patent/US11479535B2/en active Active
-
2022
- 2022-10-24 US US17/972,220 patent/US12202807B2/en active Active
-
2024
- 2024-12-12 US US18/978,238 patent/US20250109109A1/en active Pending
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