ES2120881B1 - ENANTIOMERS OF 5-METHYL-1, 3-TIAZIN-2, 4-DIONA AND ITS USE IN THE INTERMEDIATE SYNTHESIS OF CHIRAL PHARMACES. - Google Patents
ENANTIOMERS OF 5-METHYL-1, 3-TIAZIN-2, 4-DIONA AND ITS USE IN THE INTERMEDIATE SYNTHESIS OF CHIRAL PHARMACES.Info
- Publication number
- ES2120881B1 ES2120881B1 ES9600265A ES9600265A ES2120881B1 ES 2120881 B1 ES2120881 B1 ES 2120881B1 ES 9600265 A ES9600265 A ES 9600265A ES 9600265 A ES9600265 A ES 9600265A ES 2120881 B1 ES2120881 B1 ES 2120881B1
- Authority
- ES
- Spain
- Prior art keywords
- enantiomers
- methyl
- chiral
- synthesis
- pharmaces
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Expired - Lifetime
Links
- 230000015572 biosynthetic process Effects 0.000 title abstract 4
- 238000003786 synthesis reaction Methods 0.000 title abstract 4
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical compound C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 title abstract 3
- RHWUNRXGCOWRKD-UHFFFAOYSA-N 5-methyl-1,3-thiazine-2,4-dione Chemical class CC1=CSC(=O)NC1=O RHWUNRXGCOWRKD-UHFFFAOYSA-N 0.000 abstract 3
- 102000004190 Enzymes Human genes 0.000 abstract 2
- 108090000790 Enzymes Proteins 0.000 abstract 2
- 239000000543 intermediate Substances 0.000 abstract 2
- 230000000707 stereoselective effect Effects 0.000 abstract 2
- 239000004480 active ingredient Substances 0.000 abstract 1
- 239000011942 biocatalyst Substances 0.000 abstract 1
- FAKRSMQSSFJEIM-RQJHMYQMSA-N captopril Chemical compound SC[C@@H](C)C(=O)N1CCC[C@H]1C(O)=O FAKRSMQSSFJEIM-RQJHMYQMSA-N 0.000 abstract 1
- 229960000830 captopril Drugs 0.000 abstract 1
- 229940079593 drug Drugs 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 230000007071 enzymatic hydrolysis Effects 0.000 abstract 1
- 238000006047 enzymatic hydrolysis reaction Methods 0.000 abstract 1
- 230000003301 hydrolyzing effect Effects 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 239000002243 precursor Substances 0.000 abstract 1
Landscapes
- Preparation Of Compounds By Using Micro-Organisms (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
Enantiomeros de 5-metil-1,3-tiazin-2,4-diona y su empleo en la síntesis de intermedios de fármacos quirales. Los enantiómeros de la 5-metil-1,3-tiazin-2,4-diona (I) son adecuados para la síntesis de intermedios de principios activos farmacéuticos quirales. En particular, el enantiómero S de (I) es útil para la síntesis del ácido S-(-)-3-acetiltio-2 metilpropiónico (S-AMPA), un precursor del Captopril. Esto enantiómeros pueden obtenerse por hidrólisis enzimática estereoselectiva de la 5-metil-1,3-tiazin-2,4-diona racémica en presencia de un biocatalizador que contiene enzimas capaces de hidrolizar dicha mezcla racémica de forma estereoselectiva.5-methyl-1,3-thiazin-2,4-dione enantiomers and their use in the synthesis of chiral drug intermediates. The enantiomers of 5-methyl-1,3-thiazin-2,4-dione (I) are suitable for the synthesis of intermediates of chiral pharmaceutical active ingredients. In particular, the S enantiomer of (I) is useful for the synthesis of S - (-) - 3-acetylthio-2-methylpropionic acid (S-AMPA), a precursor to Captopril. These enantiomers can be obtained by stereoselective enzymatic hydrolysis of racemic 5-methyl-1,3-thiazin-2,4-dione in the presence of a biocatalyst containing enzymes capable of hydrolyzing said racemic mixture in a stereoselective manner.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| ES9600265A ES2120881B1 (en) | 1996-02-05 | 1996-02-05 | ENANTIOMERS OF 5-METHYL-1, 3-TIAZIN-2, 4-DIONA AND ITS USE IN THE INTERMEDIATE SYNTHESIS OF CHIRAL PHARMACES. |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| ES9600265A ES2120881B1 (en) | 1996-02-05 | 1996-02-05 | ENANTIOMERS OF 5-METHYL-1, 3-TIAZIN-2, 4-DIONA AND ITS USE IN THE INTERMEDIATE SYNTHESIS OF CHIRAL PHARMACES. |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| ES2120881A1 ES2120881A1 (en) | 1998-11-01 |
| ES2120881B1 true ES2120881B1 (en) | 1999-11-16 |
Family
ID=8293694
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES9600265A Expired - Lifetime ES2120881B1 (en) | 1996-02-05 | 1996-02-05 | ENANTIOMERS OF 5-METHYL-1, 3-TIAZIN-2, 4-DIONA AND ITS USE IN THE INTERMEDIATE SYNTHESIS OF CHIRAL PHARMACES. |
Country Status (1)
| Country | Link |
|---|---|
| ES (1) | ES2120881B1 (en) |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA1318627C (en) * | 1988-07-14 | 1993-06-01 | Jeffrey M. Howell | Enzymatic resolution process |
| US5128263A (en) * | 1988-07-14 | 1992-07-07 | E. R. Squibb & Sons, Inc. | Enzymatic resolution process hydrolyzing thio-ester |
| US5177006A (en) * | 1988-07-14 | 1993-01-05 | E. R. Squibb & Sons, Inc. | Enzymatic resolution process |
| NL8802849A (en) * | 1988-11-18 | 1990-06-18 | Stamicarbon | PROCESS FOR THE ENANTIOSELECTIVE PREPARATION OF D - (-) - 3-HAL-METHYL-PROPIONIC ACID OR DERIVATIVES THEREOF AND THE PREPARATION OF CAPTOPRIL THEREOF |
-
1996
- 1996-02-05 ES ES9600265A patent/ES2120881B1/en not_active Expired - Lifetime
Also Published As
| Publication number | Publication date |
|---|---|
| ES2120881A1 (en) | 1998-11-01 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| PC2A | Transfer granted | ||
| EC2A | Search report published |
Date of ref document: 19981101 Kind code of ref document: A1 Effective date: 19981101 |
|
| FA2A | Application withdrawn |
Effective date: 20001030 |