AR043505A1 - PREPARATION OF BETA-CETOAMIDS AND REACTION INTERMEDIARIES - Google Patents
PREPARATION OF BETA-CETOAMIDS AND REACTION INTERMEDIARIESInfo
- Publication number
- AR043505A1 AR043505A1 ARP040100731A AR043505A1 AR 043505 A1 AR043505 A1 AR 043505A1 AR P040100731 A ARP040100731 A AR P040100731A AR 043505 A1 AR043505 A1 AR 043505A1
- Authority
- AR
- Argentina
- Prior art keywords
- preparation
- unsubstituted
- structural formula
- substituted
- cetoamids
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 abstract 3
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 2
- KYQCOXFCLRTKLS-UHFFFAOYSA-N Pyrazine Chemical compound C1=CN=CC=N1 KYQCOXFCLRTKLS-UHFFFAOYSA-N 0.000 abstract 2
- 239000002253 acid Substances 0.000 abstract 2
- 229910052736 halogen Inorganic materials 0.000 abstract 2
- 125000005843 halogen group Chemical group 0.000 abstract 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 2
- 125000001424 substituent group Chemical group 0.000 abstract 2
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 abstract 2
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 2
- NSPMIYGKQJPBQR-UHFFFAOYSA-N 4H-1,2,4-triazole Chemical compound C=1N=CNN=1 NSPMIYGKQJPBQR-UHFFFAOYSA-N 0.000 abstract 1
- PCNDJXKNXGMECE-UHFFFAOYSA-N Phenazine Natural products C1=CC=CC2=NC3=CC=CC=C3N=C21 PCNDJXKNXGMECE-UHFFFAOYSA-N 0.000 abstract 1
- 239000003960 organic solvent Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Reivindicación 1: Procedimiento para la preparación de un compuesto de fórmula estructural (1) en la que R1 es un H o un alquilo C1-4 no sustituido o sustituido conde 1 a 5 F; que comprende el paso de tratar un compuesto de fórmula estructural (2) en la que Ar es un fenilo que no está sustituido o que está sustituido con de 1 a 5 sustituyentes seleccionados independientemente del grupo constituido por halógeno, trifluorometilo y trifluorometoxi, con una 5,6,7,8-tetrahidro[1,2,4]-triazol[4,3-a]pirazina de fórmula estructural (5) o una sal ácida de la misma en presencia de un ácido o base en un disolvente orgánico apropiado. Reivindicación 9: Compuesto de fórmula estructural (1) en el que Ar es un fenilo que no está sustituido o que está sustituido con e 1 a 5 sustituyentes seleccionados independientemente del grupo constituido por halógeno, trifluorometilo y trifluorometoxi; y R1 es un H o un alquilo C1-4 no sustituido o sustituido con de 1 a 5 F.Claim 1: Process for the preparation of a compound of structural formula (1) wherein R1 is an H or an unsubstituted C1-4 alkyl substituted from 1 to 5 F; comprising the step of treating a compound of structural formula (2) in which Ar is a phenyl that is unsubstituted or that is substituted with 1 to 5 substituents independently selected from the group consisting of halogen, trifluoromethyl and trifluoromethoxy, with a , 6,7,8-tetrahydro [1,2,4] -triazol [4,3-a] pyrazine of structural formula (5) or an acid salt thereof in the presence of an acid or base in an appropriate organic solvent . Claim 9: Compound of structural formula (1) wherein Ar is a phenyl that is unsubstituted or substituted with e 1 to 5 substituents independently selected from the group consisting of halogen, trifluoromethyl and trifluoromethoxy; and R1 is an H or a C1-4 alkyl unsubstituted or substituted with 1 to 5 F.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US45545803P | 2003-03-18 | 2003-03-18 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR043505A1 true AR043505A1 (en) | 2005-08-03 |
Family
ID=33030004
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP040100731 AR043505A1 (en) | 2003-03-18 | 2004-03-08 | PREPARATION OF BETA-CETOAMIDS AND REACTION INTERMEDIARIES |
Country Status (3)
| Country | Link |
|---|---|
| AR (1) | AR043505A1 (en) |
| TW (1) | TW200505923A (en) |
| WO (1) | WO2004083212A1 (en) |
Families Citing this family (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| HUP0400321A2 (en) | 2001-06-27 | 2004-08-30 | Smithkline Beecham Corp. | Fluoropyrrolidines as dipeptidyl peptidase inhibitors and pharmaceutical compositions containing them |
| US7550590B2 (en) | 2003-03-25 | 2009-06-23 | Takeda Pharmaceutical Company Limited | Dipeptidyl peptidase inhibitors |
| EP1625122A1 (en) | 2003-05-14 | 2006-02-15 | Takeda San Diego, Inc. | Dipeptidyl peptidase inhibitors |
| ZA200602051B (en) | 2003-08-13 | 2007-10-31 | Takeda Pharmaceutical | 4-pyrimidone derivatives and their use as peptidyl peptidase inhibitors |
| CN101087756B (en) | 2004-07-23 | 2011-04-06 | 纽阿达有限责任公司 | Peptidase inhibitors |
| ZA200802857B (en) | 2005-09-14 | 2009-09-30 | Takeda Pharmaceutical | Dipeptidyl peptidase inhibitors for treating diabetes |
| CN101360723A (en) | 2005-09-16 | 2009-02-04 | 武田药品工业株式会社 | Process for preparing pyrimidinedione derivatives |
| US20090156465A1 (en) | 2005-12-30 | 2009-06-18 | Sattigeri Jitendra A | Derivatives of beta-amino acid as dipeptidyl peptidase-iv inhibitors |
| WO2007112347A1 (en) | 2006-03-28 | 2007-10-04 | Takeda Pharmaceutical Company Limited | Dipeptidyl peptidase inhibitors |
| TW200838536A (en) | 2006-11-29 | 2008-10-01 | Takeda Pharmaceutical | Polymorphs of succinate salt of 2-[6-(3-amino-piperidin-1-yl)-3-methyl-2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-ylmethy]-4-fluor-benzonitrile and methods of use therefor |
| EP2726484A1 (en) | 2011-06-29 | 2014-05-07 | Ranbaxy Laboratories Limited | Solid dispersions of sitagliptin and processes for their preparation |
| AU2012277403A1 (en) | 2011-06-30 | 2014-01-30 | Ranbaxy Laboratories Limited | Novel salts of sitagliptin |
| US20140350023A1 (en) | 2011-12-08 | 2014-11-27 | Ranbaxy Laboratories Limited | Amorphous form of sitagliptin salts |
| CN116199691A (en) * | 2022-09-01 | 2023-06-02 | 淄博矿业集团有限责任公司 | Synthesis method of sitagliptin important intermediate |
| EP4630568A1 (en) | 2022-12-09 | 2025-10-15 | KRKA, D.D., Novo Mesto | Process for the preparation of sitagliptin |
| CN116284004A (en) * | 2023-03-29 | 2023-06-23 | 宙晟智维生命科学(上海)有限公司 | A kind of continuous method for synthesizing sitagliptin phosphate intermediate |
Family Cites Families (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| UA74912C2 (en) * | 2001-07-06 | 2006-02-15 | Merck & Co Inc | Beta-aminotetrahydroimidazo-(1,2-a)-pyrazines and tetratriazolo-(4,3-a)-pyrazines as inhibitors of dipeptylpeptidase for the treatment or prevention of diabetes |
-
2004
- 2004-03-08 AR ARP040100731 patent/AR043505A1/en not_active Application Discontinuation
- 2004-03-12 WO PCT/US2004/007834 patent/WO2004083212A1/en not_active Ceased
- 2004-03-17 TW TW093107081A patent/TW200505923A/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| WO2004083212A1 (en) | 2004-09-30 |
| TW200505923A (en) | 2005-02-16 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure | ||
| FA | Abandonment or withdrawal | ||
| FA | Abandonment or withdrawal |