AR003831A1 - IMPROVED PROCEDURE TO PRODUCE EPTASTIGMINE AND A NEW INTERMEDIATE USEFUL TO THIS END. - Google Patents
IMPROVED PROCEDURE TO PRODUCE EPTASTIGMINE AND A NEW INTERMEDIATE USEFUL TO THIS END.Info
- Publication number
- AR003831A1 AR003831A1 ARP960104662A ARP960104662A AR003831A1 AR 003831 A1 AR003831 A1 AR 003831A1 AR P960104662 A ARP960104662 A AR P960104662A AR P960104662 A ARP960104662 A AR P960104662A AR 003831 A1 AR003831 A1 AR 003831A1
- Authority
- AR
- Argentina
- Prior art keywords
- eptastigmine
- produce
- new intermediate
- improved procedure
- intermediate useful
- Prior art date
Links
- RRGMXBQMCUKRLH-CTNGQTDRSA-N [(3ar,8bs)-3,4,8b-trimethyl-2,3a-dihydro-1h-pyrrolo[2,3-b]indol-7-yl] n-heptylcarbamate Chemical compound C12=CC(OC(=O)NCCCCCCC)=CC=C2N(C)[C@@H]2[C@@]1(C)CCN2C RRGMXBQMCUKRLH-CTNGQTDRSA-N 0.000 title abstract 2
- 229950010753 eptastigmine Drugs 0.000 title abstract 2
- PIJVFDBKTWXHHD-UHFFFAOYSA-N Physostigmine Natural products C12=CC(OC(=O)NC)=CC=C2N(C)C2C1(C)CCN2C PIJVFDBKTWXHHD-UHFFFAOYSA-N 0.000 abstract 2
- HKGWQUVGHPDEBZ-OLZOCXBDSA-N eseroline Chemical compound C1=C(O)C=C2[C@]3(C)CCN(C)[C@@H]3N(C)C2=C1 HKGWQUVGHPDEBZ-OLZOCXBDSA-N 0.000 abstract 2
- PIJVFDBKTWXHHD-HIFRSBDPSA-N physostigmine Chemical compound C12=CC(OC(=O)NC)=CC=C2N(C)[C@@H]2[C@@]1(C)CCN2C PIJVFDBKTWXHHD-HIFRSBDPSA-N 0.000 abstract 2
- 229960001697 physostigmine Drugs 0.000 abstract 2
- 125000003808 silyl group Chemical group [H][Si]([H])([H])[*] 0.000 abstract 2
- 239000002253 acid Substances 0.000 abstract 1
- 239000003795 chemical substances by application Substances 0.000 abstract 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 1
- 150000007524 organic acids Chemical class 0.000 abstract 1
- 235000005985 organic acids Nutrition 0.000 abstract 1
- 239000003880 polar aprotic 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)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Procedimiento mejorado para producir eptastigmina y sus sales de adición ácida con ácidos orgánicos en el cual la mejora consiste en el hecho de que lapreparación de eserolina a partir de fisostigmina se realiza haciendo reaccionar la fisostigmina con un agente sililante adecuado y sustituyendodespués, en el silil derivado así obtenido, el grupo sililo por un átomo de hidrógeno. Ventajosamente, la sucesiva adición de eptilisocianato a laeserolina se realiza en presencia de una base y de un solvente polar aprótico.Improved process to produce eptastigmine and its acid addition salts with organic acids, in which the improvement consists in the fact that the preparation of eseroline from physostigmine is carried out by reacting the physostigmine with a suitable silylating agent and then substituting, in the silyl derived thus obtained, the silyl group for a hydrogen atom. Advantageously, the successive addition of eptylisocyanate to eseroline is carried out in the presence of a base and a polar aprotic solvent.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| IT95MI002097A IT1276928B1 (en) | 1995-10-13 | 1995-10-13 | IMPROVED PROCESS TO PRODUCE EPTASTIGMINE AND NEW INTERMEDIATE USEFUL FOR THE PURPOSE |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR003831A1 true AR003831A1 (en) | 1998-09-09 |
Family
ID=11372353
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP960104662A AR003831A1 (en) | 1995-10-13 | 1996-10-09 | IMPROVED PROCEDURE TO PRODUCE EPTASTIGMINE AND A NEW INTERMEDIATE USEFUL TO THIS END. |
Country Status (5)
| Country | Link |
|---|---|
| AR (1) | AR003831A1 (en) |
| AU (1) | AU7284196A (en) |
| IT (1) | IT1276928B1 (en) |
| WO (1) | WO1997014694A1 (en) |
| ZA (1) | ZA968284B (en) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2543322A1 (en) | 2003-10-21 | 2005-05-12 | Sention, Inc. | Carbamoyl esters that inhibit cholinesterase and release pharmacologically active agents |
| MX2009008288A (en) | 2007-02-02 | 2009-12-01 | Colucid Pharmaceuticals Inc | Compounds that inhibit cholinesterase. |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IT1199076B (en) * | 1984-03-01 | 1988-12-30 | Consiglio Nazionale Ricerche | PHYSOSTIGMINE DERIVATIVES WITH PROPERTY OF INHIBITION OF ACETICOLINESTERASI AND RELATED PRODUCTION PROCESS |
| IT1225462B (en) * | 1987-04-03 | 1990-11-14 | Mediolanum Farmaceutici Srl | ORGANIC SALTS OF PHYSOSTIGMIN DERIVATIVES |
| IT1244746B (en) * | 1991-02-14 | 1994-08-08 | Laboratorio Chimico Int Spa | PROCEDURE FOR THE PREPARATION OF 1,3A, 8, -TRIMETHYL-1,2,3,3A, 8, -8A-HEXAIDRO PIRROL (2,3-B) INDOLO-5 (3AS, 8AR) -EPTILCARBAMMATE |
-
1995
- 1995-10-13 IT IT95MI002097A patent/IT1276928B1/en active IP Right Grant
-
1996
- 1996-10-02 WO PCT/EP1996/004296 patent/WO1997014694A1/en not_active Ceased
- 1996-10-02 AU AU72841/96A patent/AU7284196A/en not_active Abandoned
- 1996-10-02 ZA ZA968284A patent/ZA968284B/en unknown
- 1996-10-09 AR ARP960104662A patent/AR003831A1/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| AU7284196A (en) | 1997-05-07 |
| ITMI952097A0 (en) | 1995-10-13 |
| ZA968284B (en) | 1997-05-02 |
| ITMI952097A1 (en) | 1997-04-13 |
| WO1997014694A1 (en) | 1997-04-24 |
| IT1276928B1 (en) | 1997-11-03 |
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