JPS5826916B2 - Manufacturing method of diphosphoglycerate - Google Patents
Manufacturing method of diphosphoglycerateInfo
- Publication number
- JPS5826916B2 JPS5826916B2 JP650780A JP650780A JPS5826916B2 JP S5826916 B2 JPS5826916 B2 JP S5826916B2 JP 650780 A JP650780 A JP 650780A JP 650780 A JP650780 A JP 650780A JP S5826916 B2 JPS5826916 B2 JP S5826916B2
- Authority
- JP
- Japan
- Prior art keywords
- jetanolamino
- bis
- pyrimidine
- diphosphoglyceric acid
- present
- 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
Links
Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Description
【発明の詳細な説明】
２・３−ジホスホグリセリン酸は微生物、植物および哺
乳動物等に広く分布し、特に鴫乳動物の赤血球に多量に
存在する。DETAILED DESCRIPTION OF THE INVENTION 2,3-diphosphoglyceric acid is widely distributed in microorganisms, plants, mammals, etc., and is particularly present in large amounts in red blood cells of mammals.
本発明はこの２・３−ジホスホグリセリン酸に２・６−
ビス−（ジェタノールアミノ）−４・８ジピペリジノピ
リミド−（５・４−ｄ）ピリミジンを反応させることに
よって相当する新規２・３−ジホスホグリセリン酸の塩
とするものである。The present invention provides 2,6-
The corresponding novel 2,3-diphosphoglyceric acid salt is prepared by reacting bis-(jetanolamino)-4,8dipiperidinopyrimido-(5,4-d)pyrimidine.
本発明によって得られる２・３−ジホスホグリセリン酸
の塩は新規な化合物であり、２・３−ジホスホグリセリ
ン酸の生理活性作用（特に血栓形成阻止作用）を相剰的
に増強するものであり、動脈血栓症、狭心症、或は動脈
硬化性疾患の治療薬として、又血液透析時の凝血防止剤
として極めて有用である。The salt of 2,3-diphosphoglyceric acid obtained by the present invention is a new compound, and it complementarily enhances the physiologically active action (particularly the antithrombotic action) of 2,3-diphosphoglyceric acid. It is extremely useful as a therapeutic agent for arterial thrombosis, angina pectoris, or arteriosclerotic disease, and as an anticoagulant during hemodialysis.
本発明によって製造される化合物の化学的性状を表１に
示す。The chemical properties of the compounds produced according to the present invention are shown in Table 1.
本発明によって得られる化合物の血小板凝集抑制効果を
以下に示す。The platelet aggregation inhibitory effects of the compounds obtained by the present invention are shown below.
Ａｇｇｒｅｇｏｍｅｔｅｒを用いた透過度の変化を第１
図ニ示した。First, change in transmittance using an aggregometer.
Figure D shows.
円形キュベツトにモルモットＰ １ａｔｅｌｅｔｒｉｃ
ｈ Ｐｌａｓｍａ（ＰＲＰ ） ０．８ｍｌ及び被検液
０．１ ｒｒＬｌ又は生食（コントロールとして） ０
．１ ｍｌを加え全量１ ｒｕｌとし、測定した。Guinea pig P 1ateletric in a circular cuvette
h Plasma (PRP) 0.8 ml and test solution 0.1 rrLl or saline (as control) 0
．． 1 ml was added to make a total volume of 1 rul, and the measurement was performed.
測定は３７°Ｃで約３０００ｐｐｍ攪拌下に行なった。Measurements were carried out at 37° C. with stirring at approximately 3000 ppm.
本発明によって得られる化合物は優れた血小板凝集抑制
作用を示し、その作用は、２・３−ジホスホグリセリン
酸と２・６−ビス−（ジェタノールアミノ）−４・８−
ジピペリジノビリミド−（５・４−ｄ）ピリミジン塩の
双方をはるかに凌駕するものである。The compound obtained according to the present invention exhibits an excellent platelet aggregation inhibitory effect, and the effect is due to the effects of 2,3-diphosphoglyceric acid and 2,6-bis-(jetanolamino)-4,8-
It far exceeds both dipiperidinopyrimide-(5.4-d)pyrimidine salt.
以下に本発明を実施例によってさらに詳細に説明する。The present invention will be explained in more detail below by way of examples.
実施例 １
２・６−ビス−（ジェタノールアミノ）−４・８−ジピ
ペリジノピリミド−（５・４−ｄ）ピリミジン５１をエ
タノール１０１ｒＬｌにとかしこの溶液に２・３−ジホ
スホグリセリン酸３１のエタノル溶液を加えると橙黄色
の結晶が析出してくる。Example 1 2,6-bis-(jetanolamino)-4,8-dipiperidinopyrimido-(5,4-d)pyrimidine 51 was dissolved in 101 rLl of ethanol, and 2,3-diphosphoglycerin was added to this solution. When an ethanol solution of acid 31 is added, orange-yellow crystals precipitate out.
多量のエタノールから再結晶すると黄色結晶として２・
３−ジホスホグリセリン酸の２・６−ビス（ジェタノー
ルアミノ）−４・８〜ジピペリジノピリミドー（５・４
−ｄ）ピリミジン塩ｍ、ｐ。When recrystallized from a large amount of ethanol, 2.
3-diphosphoglyceric acid 2,6-bis(jetanolamino)-4,8~dipiperidinopyrimide (5,4
-d) Pyrimidine salts m, p.
２５０℃以上（分解）６グが得られる。At 250°C or higher (decomposition), 6 grams are obtained.
第１図はモルモット血小板凝集に対する２・３−ジホス
ホグリセリン酸の２・６−ビス−（ジェタノールアミノ
）−４・８−ジピペリジノピリミド−（５・４−ｄ）ピ
リミジン塩の作用を示す。
図中、１はコントロール、２は２・３−ジホスホグリセ
リン酸（５０μｌ）、３は２・６−ビス−（ジェタノー
ルアミノ）−４・８−ジピペリジノピリミド−（５・４
−ｄ）ピリミジン（１００μｍ）、４はジホスホグリセ
リン酸の２−６−ビス−（ジェタノールアミノ）−４・
８−ジピリジノピリミドー（５・４−ｄ）ピリミジン塩
（５０μグ）を表わす。
矢印はノルエピネフリン（５μＭ）を添加した時点を表
わす。Figure 1 shows the effect of 2,6-bis-(jetanolamino)-4,8-dipiperidinopyrimide-(5,4-d)pyrimidine salt of 2,3-diphosphoglyceric acid on guinea pig platelet aggregation. Show action. In the figure, 1 is the control, 2 is 2,3-diphosphoglyceric acid (50 μl), and 3 is 2,6-bis-(jetanolamino)-4,8-dipiperidinopyrimide-(5,4
-d) Pyrimidine (100 μm), 4 is diphosphoglyceric acid 2-6-bis-(jetanolamino)-4.
Represents 8-dipyridinopyrimide (5.4-d) pyrimidine salt (50 μg). Arrows indicate the time point when norepinephrine (5 μM) was added.
Claims (1)
ジェタノールアミノ）−４・８−ジピペ※※リジノピリ
ミド−（５・４−ｄ）ピリミジンを反応させることより
成る２・３−ジホスホグリセリン酸の有機アミン塩の製
造法。12,3-diphosphoglyceric acid, 2,6-bis-(
A method for producing an organic amine salt of 2,3-diphosphoglyceric acid, which comprises reacting jetanolamino)-4,8-dipipe**lysinopyrimide-(5,4-d)pyrimidine.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP650780A JPS5826916B2 (en) | 1980-01-22 | 1980-01-22 | Manufacturing method of diphosphoglycerate |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP650780A JPS5826916B2 (en) | 1980-01-22 | 1980-01-22 | Manufacturing method of diphosphoglycerate |
Related Parent Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP3374775A Division JPS51108020A (en) | 1975-03-20 | 1975-03-20 | 2*33 jihosuhoguriserinsanno jukiaminenruinoseiho |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JPS55147295A JPS55147295A (en) | 1980-11-17 |
| JPS5826916B2 true JPS5826916B2 (en) | 1983-06-06 |
Family
ID=11640335
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP650780A Expired JPS5826916B2 (en) | 1980-01-22 | 1980-01-22 | Manufacturing method of diphosphoglycerate |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JPS5826916B2 (en) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2002010177A1 (en) | 2000-08-01 | 2002-02-07 | Gmp Companies, Inc. | Ammonium salts of inositol hexaphosphate and uses thereof |
| WO2002009723A2 (en) * | 2000-08-01 | 2002-02-07 | Gmp Companies, Inc. | Ammonium salts of hemoglobin allosteric effectors, and uses thereof |
-
1980
- 1980-01-22 JP JP650780A patent/JPS5826916B2/en not_active Expired
Also Published As
| Publication number | Publication date |
|---|---|
| JPS55147295A (en) | 1980-11-17 |
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