KR830005233A - 6-[d(-)-알파-(4-c_1~c_4)알킬-2,3-디옥소-1-피페라지노 카르보닐아미노)페닐아세트아미도] 페니실란산 제조방법 - Google Patents
6-[d(-)-알파-(4-c_1~c_4)알킬-2,3-디옥소-1-피페라지노 카르보닐아미노)페닐아세트아미도] 페니실란산 제조방법 Download PDFInfo
- Publication number
- KR830005233A KR830005233A KR1019810001331A KR810001331A KR830005233A KR 830005233 A KR830005233 A KR 830005233A KR 1019810001331 A KR1019810001331 A KR 1019810001331A KR 810001331 A KR810001331 A KR 810001331A KR 830005233 A KR830005233 A KR 830005233A
- Authority
- KR
- South Korea
- Prior art keywords
- added
- ampicillin
- dioxo
- alkyl
- parts
- Prior art date
Links
- 239000002253 acid Substances 0.000 title claims 3
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 title 1
- XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 claims 12
- AVKUERGKIZMTKX-NJBDSQKTSA-N ampicillin Chemical compound C1([C@@H](N)C(=O)N[C@H]2[C@H]3SC([C@@H](N3C2=O)C(O)=O)(C)C)=CC=CC=C1 AVKUERGKIZMTKX-NJBDSQKTSA-N 0.000 claims 7
- 229960000723 ampicillin Drugs 0.000 claims 7
- 239000011541 reaction mixture Substances 0.000 claims 6
- 239000000203 mixture Substances 0.000 claims 4
- 238000003756 stirring Methods 0.000 claims 3
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 3
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 2
- -1 carbonyl halide Chemical class 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- 239000000725 suspension Substances 0.000 claims 2
- 150000004820 halides Chemical class 0.000 claims 1
- 239000002198 insoluble material Substances 0.000 claims 1
- 239000012452 mother liquor Substances 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 239000011877 solvent mixture Substances 0.000 claims 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D499/00—Heterocyclic compounds containing 4-thia-1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula:, e.g. penicillins, penems; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulfur-containing hetero ring
- C07D499/21—Heterocyclic compounds containing 4-thia-1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula:, e.g. penicillins, penems; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulfur-containing hetero ring with a nitrogen atom directly attached in position 6 and a carbon atom having three bonds to hetero atoms with at the most one bond to halogen, e.g. an ester or nitrile radical, directly attached in position 2
- C07D499/28—Heterocyclic compounds containing 4-thia-1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula:, e.g. penicillins, penems; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulfur-containing hetero ring with a nitrogen atom directly attached in position 6 and a carbon atom having three bonds to hetero atoms with at the most one bond to halogen, e.g. an ester or nitrile radical, directly attached in position 2 with modified 2-carboxyl group
- C07D499/32—Esters
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
내용 없음
Description
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음
Claims (1)
- 염기 존재하에 아세트산 에틸과 물로 된 혼합물에 첨가한 암피실린 현탁물 또는 용액에 4-C1-C4알킬-2,3-디옥소-1-피페라지노 카르보닐 할로겐화물을 첨가하여 반응혼합물을 만들어 반응이 완료될 때까지 교반하고 반응혼합물을 산성화한 후 경정질 생성물을 회수하므로서 6-[D(-)-알파-(4-C1-C4알킬-2,3-디옥소-1-피페라지노카르보닐아미노)페닐아세트아미도] 페니실란산을 제조하는 방법에 있어서 :(1) 암피실린 중량부당 아세트산 에틸 약 0.5-8중량부와 물 약 9-12중량부로 된 용매 혼합물에 적당량의 적절한 염기 및 약 1몰 정도의 암피실린을 가하여 교반해서 된 현탁물에다 약 1-1.5몰 정도의 4-C1-C4알킬-2,3-디옥소-1-피페라지노 카르보닐 할로겐화물을 pH를 약 6-8.3으로 유지하면서 최소한 30분 정도에 걸쳐 첨가하고,(2) (1)단계에서 4-C1-C4알킬-2,3-디옥소-1-피페라지노 카르보닐 할로겐화물의 첨가가 완료되면 반응 혼합물을 약 10-25℃에서 최소한 15분간 다시 교반하며,(3) (1)단계에서 첨가된 암피실린 중량부당 여과조제 및 활성탄을 각각 0.05-0.2중량부를 반응 혼합물에 첨가하고 약 10-25℃에서 최소한 10분간 교반하고,(4) 반응혼합물을 정제하여 (1)단계에서 첨가된 암피실린 중량부당 물 약 0.6-2.5중량부를 사용하여 불용물질을 세척하고,(5) (1)단계에서 첨가된 암피실린 중량부당 아세트산에틸 약 2-12.5중량부와 (4)단계에서 얻은 세척액과 모액을 혼합하는데, 이때 (1)단계와 (5)단계에서 사용되는 아세트산 에틸의 전체량을 암피실린 중량부당 약 10-13중량부로 한다. 생성된 반응혼합물을 약 15-25℃로 가열하고,(6) (5)단계에서 얻은 혼합물을 pH 약 2.0-25이 되게 산성화하며,(7) 산성화된 혼합물을 약 15-25℃에서 최소한 1시간 교반한 후 생성된 결정질 생성물을 수거하며,(8) 임의적으로 약학적으로 섭취가 가능한 염으로 전환시킴을 특징으로 하는 6-[D(-)-알파-(4-C1-C4알킬-2,3-디옥소-1-피페라지노카르보닐아미노)페닐아세트아미도] 페니실란산 제조방법.※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| KR1019810001331A KR850000611B1 (ko) | 1981-04-18 | 1981-04-18 | 6-[d(-)-알파-(4-c₁~c₄)알킬-2,3-디옥소-1-피페라지노 카르보닐아미노)페닐아세트아미도] 페니실란산 제조방법 |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| KR1019810001331A KR850000611B1 (ko) | 1981-04-18 | 1981-04-18 | 6-[d(-)-알파-(4-c₁~c₄)알킬-2,3-디옥소-1-피페라지노 카르보닐아미노)페닐아세트아미도] 페니실란산 제조방법 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| KR830005233A true KR830005233A (ko) | 1983-08-03 |
| KR850000611B1 KR850000611B1 (ko) | 1985-05-01 |
Family
ID=19220725
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1019810001331A KR850000611B1 (ko) | 1981-04-18 | 1981-04-18 | 6-[d(-)-알파-(4-c₁~c₄)알킬-2,3-디옥소-1-피페라지노 카르보닐아미노)페닐아세트아미도] 페니실란산 제조방법 |
Country Status (1)
| Country | Link |
|---|---|
| KR (1) | KR850000611B1 (ko) |
-
1981
- 1981-04-18 KR KR1019810001331A patent/KR850000611B1/ko active
Also Published As
| Publication number | Publication date |
|---|---|
| KR850000611B1 (ko) | 1985-05-01 |
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