JPS5645471A - Vitamin-e ester of tranexamic acid and its preparation - Google Patents
Vitamin-e ester of tranexamic acid and its preparationInfo
- Publication number
- JPS5645471A JPS5645471A JP12014179A JP12014179A JPS5645471A JP S5645471 A JPS5645471 A JP S5645471A JP 12014179 A JP12014179 A JP 12014179A JP 12014179 A JP12014179 A JP 12014179A JP S5645471 A JPS5645471 A JP S5645471A
- Authority
- JP
- Japan
- Prior art keywords
- acid
- ester
- vitamin
- tranexamic acid
- tranexamic
- 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.)
- Granted
Links
- GYDJEQRTZSCIOI-LJGSYFOKSA-N tranexamic acid Chemical compound NC[C@H]1CC[C@H](C(O)=O)CC1 GYDJEQRTZSCIOI-LJGSYFOKSA-N 0.000 title abstract 6
- 229960000401 tranexamic acid Drugs 0.000 title abstract 6
- 150000002148 esters Chemical class 0.000 title abstract 2
- GVJHHUAWPYXKBD-UHFFFAOYSA-N d-alpha-tocopherol Natural products OC1=C(C)C(C)=C2OC(CCCC(C)CCCC(C)CCCC(C)C)(C)CCC2=C1C GVJHHUAWPYXKBD-UHFFFAOYSA-N 0.000 abstract 4
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 abstract 3
- YMWUJEATGCHHMB-UHFFFAOYSA-N Dichloromethane Chemical compound ClCCl YMWUJEATGCHHMB-UHFFFAOYSA-N 0.000 abstract 3
- 229930003427 Vitamin E Natural products 0.000 abstract 3
- WIGCFUFOHFEKBI-UHFFFAOYSA-N gamma-tocopherol Natural products CC(C)CCCC(C)CCCC(C)CCCC1CCC2C(C)C(O)C(C)C(C)C2O1 WIGCFUFOHFEKBI-UHFFFAOYSA-N 0.000 abstract 3
- 229940046009 vitamin E Drugs 0.000 abstract 3
- 235000019165 vitamin E Nutrition 0.000 abstract 3
- 239000011709 vitamin E Substances 0.000 abstract 3
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 abstract 2
- NBIIXXVUZAFLBC-UHFFFAOYSA-N Phosphoric acid Chemical compound OP(O)(O)=O NBIIXXVUZAFLBC-UHFFFAOYSA-N 0.000 abstract 2
- -1 Vitamin E ester Chemical class 0.000 abstract 2
- 239000002253 acid Substances 0.000 abstract 2
- 238000006243 chemical reaction Methods 0.000 abstract 2
- JVTAAEKCZFNVCJ-UHFFFAOYSA-N lactic acid Chemical compound CC(O)C(O)=O JVTAAEKCZFNVCJ-UHFFFAOYSA-N 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- 239000002904 solvent Substances 0.000 abstract 2
- QOSSAOTZNIDXMA-UHFFFAOYSA-N Dicylcohexylcarbodiimide Chemical compound C1CCCCC1N=C=NC1CCCCC1 QOSSAOTZNIDXMA-UHFFFAOYSA-N 0.000 abstract 1
- 102000035195 Peptidases Human genes 0.000 abstract 1
- 108091005804 Peptidases Proteins 0.000 abstract 1
- 208000007536 Thrombosis Diseases 0.000 abstract 1
- 150000008065 acid anhydrides Chemical class 0.000 abstract 1
- 229910000147 aluminium phosphate Inorganic materials 0.000 abstract 1
- 125000003277 amino group Chemical group 0.000 abstract 1
- 239000004019 antithrombin Substances 0.000 abstract 1
- 238000009835 boiling Methods 0.000 abstract 1
- 239000003795 chemical substances by application Substances 0.000 abstract 1
- 230000032050 esterification Effects 0.000 abstract 1
- 238000005886 esterification reaction Methods 0.000 abstract 1
- 150000004820 halides Chemical class 0.000 abstract 1
- 230000002401 inhibitory effect Effects 0.000 abstract 1
- 239000004310 lactic acid Substances 0.000 abstract 1
- 235000014655 lactic acid Nutrition 0.000 abstract 1
- 239000000463 material Substances 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 150000007522 mineralic acids Chemical class 0.000 abstract 1
- 150000007524 organic acids Chemical class 0.000 abstract 1
- 230000003449 preventive effect Effects 0.000 abstract 1
- 229940024999 proteolytic enzymes for treatment of wounds and ulcers Drugs 0.000 abstract 1
Landscapes
- Pyrane Compounds (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
NEW MATERIAL:Vitamin E ester of tranexamic acid and an acid addition salt thereof.
USE: A preventive and remedy for thrombosis having improved inhibitory action on proteolytic enzymes, particulaly a selective antithrombin action.
PROCESS: Tranexamic acid or a reactive derivative thereof, preferably an acid halide or mixed acid anhydride, is reated with vitamin E, preferably in a solvent which will not take part in the reaction, e.g. dichloromethane, at room tempeature to the boiling point of the solvent for 1W3hr, to give vitamin E ester of tranexamic acid. The ester may be converted into a salt of an inorganic acid, e.g. hydrochloric or phosphoric acid, or an organic acid, e.g. acetic or lactic acid if desired. In case the tranexamic acid is directly used, a condensing agent, e.g. dicyclohexylcarbodiimide, is preferably present in the reaction system. The amino group of the tranexamic acid may be protected and then removed after esterification.
COPYRIGHT: (C)1981,JPO&Japio
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP12014179A JPS5645471A (en) | 1979-09-20 | 1979-09-20 | Vitamin-e ester of tranexamic acid and its preparation |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP12014179A JPS5645471A (en) | 1979-09-20 | 1979-09-20 | Vitamin-e ester of tranexamic acid and its preparation |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JPS5645471A true JPS5645471A (en) | 1981-04-25 |
| JPS6330905B2 JPS6330905B2 (en) | 1988-06-21 |
Family
ID=14778973
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP12014179A Granted JPS5645471A (en) | 1979-09-20 | 1979-09-20 | Vitamin-e ester of tranexamic acid and its preparation |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JPS5645471A (en) |
-
1979
- 1979-09-20 JP JP12014179A patent/JPS5645471A/en active Granted
Also Published As
| Publication number | Publication date |
|---|---|
| JPS6330905B2 (en) | 1988-06-21 |
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