SU1708345A1 - Central analgesic drug benzofurocaine - Google Patents
Central analgesic drug benzofurocaine Download PDFInfo
- Publication number
- SU1708345A1 SU1708345A1 SU813282927A SU3282927A SU1708345A1 SU 1708345 A1 SU1708345 A1 SU 1708345A1 SU 813282927 A SU813282927 A SU 813282927A SU 3282927 A SU3282927 A SU 3282927A SU 1708345 A1 SU1708345 A1 SU 1708345A1
- Authority
- SU
- USSR - Soviet Union
- Prior art keywords
- benzofurocaine
- analgesic drug
- central analgesic
- methyl
- analgesic
- Prior art date
Links
- RKXLAVAJHYGCIR-UHFFFAOYSA-N 4-chloro-6-[(dimethylazaniumyl)methyl]-3-ethoxycarbonyl-2-methyl-1-benzofuran-5-olate;2,3-dihydroxybutanedioic acid Chemical compound OC(=O)C(O)C(O)C(O)=O.CN(C)CC1=C(O)C(Cl)=C2C(C(=O)OCC)=C(C)OC2=C1 RKXLAVAJHYGCIR-UHFFFAOYSA-N 0.000 title 1
- 229940035676 analgesics Drugs 0.000 title 1
- 239000000730 antalgic agent Substances 0.000 title 1
- 230000000202 analgesic effect Effects 0.000 claims description 4
- 239000003814 drug Substances 0.000 claims description 3
- 238000000034 method Methods 0.000 claims description 3
- -1 6-dimethylaminomethyl-2-methyl-6-hydroxy-4-chlorobenzofuran-3-carboxylic acid ethyl sulfate tartrate Chemical compound 0.000 claims description 2
- 241000700159 Rattus Species 0.000 claims description 2
- 229940079593 drug Drugs 0.000 claims description 2
- 230000000638 stimulation Effects 0.000 claims description 2
- GOZBHBFUQHMKQB-UHFFFAOYSA-N trimecaine Chemical compound CCN(CC)CC(=O)NC1=C(C)C=C(C)C=C1C GOZBHBFUQHMKQB-UHFFFAOYSA-N 0.000 claims description 2
- RMMXTBMQSGEXHJ-UHFFFAOYSA-N Aminophenazone Chemical compound O=C1C(N(C)C)=C(C)N(C)N1C1=CC=CC=C1 RMMXTBMQSGEXHJ-UHFFFAOYSA-N 0.000 claims 1
- 229960000212 aminophenazone Drugs 0.000 claims 1
- 238000007920 subcutaneous administration Methods 0.000 claims 1
- 229950002569 trimecaine Drugs 0.000 claims 1
- 230000000694 effects Effects 0.000 description 4
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 3
- FEWJPZIEWOKRBE-JCYAYHJZSA-N Dextrotartaric acid Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O FEWJPZIEWOKRBE-JCYAYHJZSA-N 0.000 description 2
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 description 2
- 230000002411 adverse Effects 0.000 description 2
- 239000003795 chemical substances by application Substances 0.000 description 2
- 239000002244 precipitate Substances 0.000 description 2
- 239000000047 product Substances 0.000 description 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 2
- RYHBNJHYFVUHQT-UHFFFAOYSA-N 1,4-Dioxane Chemical compound C1COCCO1 RYHBNJHYFVUHQT-UHFFFAOYSA-N 0.000 description 1
- FEWJPZIEWOKRBE-UHFFFAOYSA-N Tartaric acid Natural products [H+].[H+].[O-]C(=O)C(O)C(O)C([O-])=O FEWJPZIEWOKRBE-UHFFFAOYSA-N 0.000 description 1
- 230000002378 acidificating effect Effects 0.000 description 1
- BJXCMMNQEALXQC-UHFFFAOYSA-N ethyl 4-chloro-5-hydroxy-2-methyl-1-benzofuran-3-carboxylate Chemical compound C1=C(O)C(Cl)=C2C(C(=O)OCC)=C(C)OC2=C1 BJXCMMNQEALXQC-UHFFFAOYSA-N 0.000 description 1
- 125000004494 ethyl ester group Chemical group 0.000 description 1
- 238000001990 intravenous administration Methods 0.000 description 1
- 229940126601 medicinal product Drugs 0.000 description 1
- 239000003960 organic solvent Substances 0.000 description 1
- 230000008533 pain sensitivity Effects 0.000 description 1
- 238000010992 reflux Methods 0.000 description 1
- 238000003756 stirring Methods 0.000 description 1
- 235000002906 tartaric acid Nutrition 0.000 description 1
- 239000011975 tartaric acid Substances 0.000 description 1
- 229940095064 tartrate Drugs 0.000 description 1
- GETQZCLCWQTVFV-UHFFFAOYSA-N trimethylamine Chemical compound CN(C)C GETQZCLCWQTVFV-UHFFFAOYSA-N 0.000 description 1
Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Description
Изобретение относитс к медицине и касаетс лекарственного средства.This invention relates to medicine and is related to a medicinal product.
Целью изобретени вл етс повышение активности действи .The aim of the invention is to increase the activity of the action.
Бензофурокаин - этиловый эфир 6-диметиламииометил-2-метил-5-окси -4-хлорбензофуран-3-карбоновой кислоты тартрат используетс в медицинской практике в виде прозрачного бесцветного раствора, имеющего кислую реакцию внутримышечно и/или внутривенно (струйно и/или капельно ).Benzofurocain - 6-dimethylammemethyl-2-methyl-5-hydroxy-4-chlorobenzofuran-3-carboxylic acid ethyl ester tartrate is used in medical practice as a clear, colorless solution, which is acidic intramuscularly and / or intravenously (jet and / or drip) .
Средство назначают по 0.1-0.3 г (10-30 мл 1%-ногЪ раствора) 1-3 раза в сутки; максимальна суточна доза 1 г(100 мл 1 %-ного раствора), внутривенно струйно бензофурокаин ввод т медленно (1 мл за 15 с).The tool is prescribed by 0.1-0.3 g (10-30 ml of 1% solution) 1-3 times a day; the maximum daily dose of 1 g (100 ml of a 1% solution), intravenous jet benzofurocain administered slowly (1 ml per 15 s).
Способ получени бензофурокаина осуществл ют следующим образом.The method of producing benzofurocain is carried out as follows.
Раствор 12,75 г 2-метил-3-карбэтокси-4хлор-5-окси6ензофурана и 8 мл 6ис(диметиламино )метана в 75 мл сухого диоксана кип т т с обратным холодильником 6ч. затем охлаждают до 20°С и выливают в воду. Выделившийс осадок отфильтровывают, промывают водой и сушат. Выход 2-метил3-карбэтокси-4-хло1 -окси-6-диметиламинометилбензофурана 12.6 г (80.5%). т.пл. 130-131.5°С (из спирта).A solution of 12.75 g of 2-methyl-3-carbethoxy-4-chloro-5-hydroxy-benzofuran and 8 ml of 6s (dimethylamino) methane in 75 ml of dry dioxane is heated under reflux for 6 hours. then cooled to 20 ° C and poured into water. The precipitate was filtered off, washed with water and dried. The yield of 2-methyl 3-carbethoxy-4-chloro-oxy-6-dimethylaminomethylbenzofuran is 12.6 g (80.5%). m.p. 130-131.5 ° C (from alcohol).
Найдено. %: С 58.10; Н 5.97; N 4.58; Ct 11.26.Found %: C 58.10; H 5.97; N 4.58; Ct 11.26.
Cl5Hl8CIN04Cl5Hl8CIN04
Вычислено. %: С 57.79; Р 5.81; N 4.49; Ct 11.39.Calculated. %: C 57.79; R 5.81; N 4.49; Ct 11.39.
Получение целевого продукта.Obtaining the target product.
К раствору 10,1 г 2-метил-З-карбэтокси4-хлор-5-окси-6-диметиламИнометилбензо фурана в безводном органическом растворителе - эфире, добавл ют при перемешивании p8CTBOpJZ,6 г винной кислоты в 25 мл спирта. Выделившийс осадок отфильтровывают из спирта. Выход целевого продукта 10 г (80%), т.пл. 164.5-166°С.To a solution of 10.1 g of 2-methyl-3-carbethoxy-4-chloro-5-hydroxy-6-dimethylammonomethylbenzo-furan in an anhydrous organic solvent, ether, is added with stirring p8CTBOpJZ, 6 g of tartaric acid in 25 ml of alcohol. The precipitate formed is filtered off from alcohol. The yield of the target product 10 g (80%), so pl. 164.5-166 ° C.
Найдено. %: С 53.02; Н 5.41.- CI 9,13.Found %: C 53.02; H 5.41.- CI 9.13.
Cl5Hl8CI04 1/2С4НбОвCl5Hl8CI04 1 / 2C4NbOv
Вычислено. %: С 52.78; Н 5.48; С19.18.Calculated. %: C, 52.78; H 5.48; S19.18.
Болеутол ющее действие препарата (подкожно) при исследовании в опытах на крысах(подкожно)по методу механического раздражени хвоста более значительно, чем у тримекаина и амидопирина, которые в исследованных дозах (20% ЛДбо) не оказывают статистически достоверных сдвигов порога болевой чувствительности (см. таблицу ). Продолжительность действи бензофурокаина составл ет 1,5-2 ч.The analgesic effect of the drug (subcutaneously) in the study in experiments on rats (subcutaneously) according to the method of mechanical stimulation of the tail is more significant than that of trimekain and amidopirin, which in the studied doses (20% of LdB) do not have statistically significant shifts in the threshold of pain sensitivity (see table). The duration of action of benzofurokain is 1.5-2 hours.
Таким образом, повышаетс активность действи средства по сравнению с известными средствами аналогичного действи . БoлeyтpJп ющee действие наблюдалось в течение 24-32 ч. побочных аффектов не наблюдаетс .Thus, the activity of the agent is increased in comparison with the known agents of the same effect. No more adverse effect was observed for 24-32 hours. No adverse affects were observed.
Claims (1)
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| SU813282927A SU1708345A1 (en) | 1981-05-12 | 1981-05-12 | Central analgesic drug benzofurocaine |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| SU813282927A SU1708345A1 (en) | 1981-05-12 | 1981-05-12 | Central analgesic drug benzofurocaine |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| SU1708345A1 true SU1708345A1 (en) | 1992-01-30 |
Family
ID=20956003
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| SU813282927A SU1708345A1 (en) | 1981-05-12 | 1981-05-12 | Central analgesic drug benzofurocaine |
Country Status (1)
| Country | Link |
|---|---|
| SU (1) | SU1708345A1 (en) |
-
1981
- 1981-05-12 SU SU813282927A patent/SU1708345A1/en active
Non-Patent Citations (1)
| Title |
|---|
| Авторское свидетельство СССР№ 486670. кл. С 07 L 5/42.1973. * |
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