AR126961A1 - Sintesis de nirogacestat - Google Patents
Sintesis de nirogacestatInfo
- Publication number
- AR126961A1 AR126961A1 ARP220102373A ARP220102373A AR126961A1 AR 126961 A1 AR126961 A1 AR 126961A1 AR P220102373 A ARP220102373 A AR P220102373A AR P220102373 A ARP220102373 A AR P220102373A AR 126961 A1 AR126961 A1 AR 126961A1
- Authority
- AR
- Argentina
- Prior art keywords
- compound
- pharmaceutically acceptable
- acceptable salt
- reacting
- under suitable
- Prior art date
Links
- VFCRKLWBYMDAED-REWPJTCUSA-N (2s)-2-[[(2s)-6,8-difluoro-1,2,3,4-tetrahydronaphthalen-2-yl]amino]-n-[1-[1-(2,2-dimethylpropylamino)-2-methylpropan-2-yl]imidazol-4-yl]pentanamide Chemical compound O=C([C@@H](N[C@@H]1CC2=C(F)C=C(F)C=C2CC1)CCC)NC1=CN(C(C)(C)CNCC(C)(C)C)C=N1 VFCRKLWBYMDAED-REWPJTCUSA-N 0.000 title abstract 3
- 229950001637 nirogacestat Drugs 0.000 title abstract 2
- 230000015572 biosynthetic process Effects 0.000 title 1
- 238000003786 synthesis reaction Methods 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 24
- 150000003839 salts Chemical class 0.000 abstract 11
- 238000000034 method Methods 0.000 abstract 7
- 238000004519 manufacturing process Methods 0.000 abstract 4
- 239000000203 mixture Substances 0.000 abstract 4
- 239000002904 solvent Substances 0.000 abstract 4
- 239000013543 active substance Substances 0.000 abstract 3
- BMYNFMYTOJXKLE-UHFFFAOYSA-N 3-azaniumyl-2-hydroxypropanoate Chemical compound NCC(O)C(O)=O BMYNFMYTOJXKLE-UHFFFAOYSA-N 0.000 abstract 2
- PFKFTWBEEFSNDU-UHFFFAOYSA-N carbonyldiimidazole Chemical compound C1=CN=CN1C(=O)N1C=CN=C1 PFKFTWBEEFSNDU-UHFFFAOYSA-N 0.000 abstract 2
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 abstract 1
- 150000007522 mineralic acids Chemical class 0.000 abstract 1
- 125000006239 protecting group Chemical group 0.000 abstract 1
- 230000002194 synthesizing effect Effects 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
- C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
- C07D233/66—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two 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, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D233/88—Nitrogen atoms, e.g. allantoin
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C227/00—Preparation of compounds containing amino and carboxyl groups bound to the same carbon skeleton
- C07C227/04—Formation of amino groups in compounds containing carboxyl groups
- C07C227/06—Formation of amino groups in compounds containing carboxyl groups by addition or substitution reactions, without increasing the number of carbon atoms in the carbon skeleton of the acid
- C07C227/08—Formation of amino groups in compounds containing carboxyl groups by addition or substitution reactions, without increasing the number of carbon atoms in the carbon skeleton of the acid by reaction of ammonia or amines with acids containing functional groups
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C227/00—Preparation of compounds containing amino and carboxyl groups bound to the same carbon skeleton
- C07C227/14—Preparation of compounds containing amino and carboxyl groups bound to the same carbon skeleton from compounds containing already amino and carboxyl groups or derivatives thereof
- C07C227/18—Preparation of compounds containing amino and carboxyl groups bound to the same carbon skeleton from compounds containing already amino and carboxyl groups or derivatives thereof by reactions involving amino or carboxyl groups, e.g. hydrolysis of esters or amides, by formation of halides, salts or esters
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C227/00—Preparation of compounds containing amino and carboxyl groups bound to the same carbon skeleton
- C07C227/26—Preparation of compounds containing amino and carboxyl groups bound to the same carbon skeleton from compounds containing carboxyl groups by reaction with HCN, or a salt thereof, and amines, or from aminonitriles
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C229/00—Compounds containing amino and carboxyl groups bound to the same carbon skeleton
- C07C229/02—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton
- C07C229/04—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated
- C07C229/06—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one amino and one carboxyl group bound to the carbon skeleton
- C07C229/10—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one amino and one carboxyl group bound to the carbon skeleton the nitrogen atom of the amino group being further bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
- C07D263/02—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
- C07D263/30—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D263/34—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three 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, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D263/44—Two oxygen atoms
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C2602/00—Systems containing two condensed rings
- C07C2602/02—Systems containing two condensed rings the rings having only two atoms in common
- C07C2602/04—One of the condensed rings being a six-membered aromatic ring
- C07C2602/10—One of the condensed rings being a six-membered aromatic ring the other ring being six-membered, e.g. tetraline
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (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)
Abstract
La presente revelación se dirige a los procesos para sintetizar (S)-2-(((S)-6,8-difluoro-1,2,3,4-tetrahidronaftalen-2-il)amino)-N-(1-(2-metil-1-(neopentilamino)propan-2-il)-1H-imidazol-4-il)pentanamida (nirogacestat). Reivindicación 1: Un proceso que comprende hacer reaccionar Compuesto (9), en un solvente con 1,1-carbonildiimidazol bajo condiciones adecuadas para formar Compuesto (10), o una sal farmacéuticamente aceptable del mismo. Reivindicación 23: Un proceso para preparar un compuesto de fórmula (V), o una sal farmacéuticamente aceptable del mismo, el proceso comprende hacer reaccionar Compuesto (12), con un compuesto de fórmula (IV), donde: LG es un grupo saliente; y PG es un grupo protector, bajo condiciones adecuadas para formar un compuesto de fórmula (V), o una sal farmacéuticamente aceptable del mismo. Reivindicación 46: Un proceso para preparar Compuesto (1), o una sal farmacéuticamente aceptable del mismo, el proceso comprende hacer reaccionar Compuesto (10), o sal farmacéuticamente aceptable del mismo, con Compuesto (11), o sal farmacéuticamente aceptable del mismo, bajo condiciones adecuadas para formar Compuesto (1), o una sal farmacéuticamente aceptable del mismo. Reivindicación 61: Un proceso que comprende hacer reaccionar Compuesto (9), en un solvente con 1,1-carbonildiimidazol bajo condiciones adecuadas para formar Compuesto (10) donde el proceso además comprende hacer reaccionar Compuesto (10) con Compuesto (11), bajo condiciones adecuadas para formar Compuesto (1), o una sal farmacéuticamente aceptable del mismo. Reivindicación 80: Un proceso que comprenden hacer reaccionar una sal farmacéuticamente aceptable de Compuesto (1), con un ácido inorgánico acuoso en un alcohol. Reivindicación 122: Un proceso para preparar una composición con un agente activo susceptible a oxidación que está sustancialmente libre de Compuesto (13), que comprende los pasos de disolver Compuesto (11) en un solvente, y combinar con Compuesto (9) para formar una mezcla que se trata con ácido bromhídrico, donde el agente activo es una sal dihidrobromuro de Compuesto (1). Reivindicación 123: Un proceso para preparar una composición que está esencialmente libre de Compuesto (13), que comprende los pasos de combinar Compuesto (10) con Compuesto (11) para formar una mezcla que se trata con ácido bromhídrico en un solvente para formar un agente activo de una sal dihidrobromuro de Compuesto (1).
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US202163239696P | 2021-09-01 | 2021-09-01 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR126961A1 true AR126961A1 (es) | 2023-12-06 |
Family
ID=85413129
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP220102373A AR126961A1 (es) | 2021-09-01 | 2022-09-01 | Sintesis de nirogacestat |
Country Status (10)
| Country | Link |
|---|---|
| US (3) | US20230089434A1 (es) |
| KR (1) | KR20240056726A (es) |
| CN (1) | CN118043305A (es) |
| AR (1) | AR126961A1 (es) |
| AU (1) | AU2022339841A1 (es) |
| CA (1) | CA3230245A1 (es) |
| CO (1) | CO2024002573A2 (es) |
| IL (1) | IL311128A (es) |
| TW (1) | TW202328068A (es) |
| WO (1) | WO2023034917A1 (es) |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2533554A1 (en) * | 2003-08-01 | 2005-02-10 | Pfizer Products Inc. | 6-membered heteroaryl compounds for the treatment of neurodegenerative disorders |
| PL1730119T3 (pl) * | 2004-03-23 | 2008-10-31 | Pfizer Products Incorporated | Związki imidazolowe do leczenia zaburzeń neurodegeneracyjnych |
| US7232820B2 (en) * | 2004-04-01 | 2007-06-19 | Pfizer Inc | Thiadiazole-amine compounds for the treatment of neurodegenerative disorders |
| WO2007034326A2 (en) * | 2005-09-22 | 2007-03-29 | Pfizer Products Inc. | Imidazole compounds for the treatment of neurological disorders |
| US10590087B1 (en) * | 2019-08-09 | 2020-03-17 | Pfizer Inc. | Solid state forms of (S)-2-(((S)-6,8-difluoro-1,2,3,4-tetrahydronaphthalen-2-yl)amino)-N-(1-(2-methyl-1-(neopentylamino)propan-2-yl)-1H-imidazol-4-yl)pentanamide and uses thereof |
-
2022
- 2022-09-01 US US17/929,153 patent/US20230089434A1/en active Pending
- 2022-09-01 CN CN202280066699.4A patent/CN118043305A/zh active Pending
- 2022-09-01 TW TW111133195A patent/TW202328068A/zh unknown
- 2022-09-01 AR ARP220102373A patent/AR126961A1/es unknown
- 2022-09-01 IL IL311128A patent/IL311128A/en unknown
- 2022-09-01 WO PCT/US2022/075839 patent/WO2023034917A1/en active Application Filing
- 2022-09-01 AU AU2022339841A patent/AU2022339841A1/en active Pending
- 2022-09-01 CA CA3230245A patent/CA3230245A1/en active Pending
- 2022-09-01 KR KR1020247009011A patent/KR20240056726A/ko unknown
- 2022-09-30 US US17/937,283 patent/US20230091415A1/en active Pending
-
2023
- 2023-04-20 US US18/304,202 patent/US20230312480A1/en active Pending
-
2024
- 2024-02-29 CO CONC2024/0002573A patent/CO2024002573A2/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| US20230312480A1 (en) | 2023-10-05 |
| CO2024002573A2 (es) | 2024-03-07 |
| CA3230245A1 (en) | 2023-03-09 |
| WO2023034917A1 (en) | 2023-03-09 |
| AU2022339841A1 (en) | 2024-03-28 |
| TW202328068A (zh) | 2023-07-16 |
| US20230089434A1 (en) | 2023-03-23 |
| CN118043305A (zh) | 2024-05-14 |
| IL311128A (en) | 2024-04-01 |
| KR20240056726A (ko) | 2024-04-30 |
| US20230091415A1 (en) | 2023-03-23 |
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