JPS5636441A - Preparation of encephaline derivative - Google Patents
Preparation of encephaline derivativeInfo
- Publication number
- JPS5636441A JPS5636441A JP11219179A JP11219179A JPS5636441A JP S5636441 A JPS5636441 A JP S5636441A JP 11219179 A JP11219179 A JP 11219179A JP 11219179 A JP11219179 A JP 11219179A JP S5636441 A JPS5636441 A JP S5636441A
- Authority
- JP
- Japan
- Prior art keywords
- derivative
- encephaline
- lower alkyl
- formula
- compound
- 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
- 125000000217 alkyl group Chemical group 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 3
- DTQVDTLACAAQTR-UHFFFAOYSA-N Trifluoroacetic acid Chemical compound OC(=O)C(F)(F)F DTQVDTLACAAQTR-UHFFFAOYSA-N 0.000 abstract 2
- 230000000202 analgesic effect Effects 0.000 abstract 2
- 239000003795 chemical substances by application Substances 0.000 abstract 2
- 125000006239 protecting group Chemical group 0.000 abstract 2
- 150000003568 thioethers Chemical class 0.000 abstract 2
- ITMCEJHCFYSIIV-UHFFFAOYSA-N triflic acid Chemical compound OS(=O)(=O)C(F)(F)F ITMCEJHCFYSIIV-UHFFFAOYSA-N 0.000 abstract 2
- 102000003840 Opioid Receptors Human genes 0.000 abstract 1
- 108090000137 Opioid Receptors Proteins 0.000 abstract 1
- 125000004453 alkoxycarbonyl group Chemical group 0.000 abstract 1
- 125000005098 aryl alkoxy carbonyl group Chemical group 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 231100000053 low toxicity Toxicity 0.000 abstract 1
- 239000003887 narcotic antagonist Substances 0.000 abstract 1
- HNKJADCVZUBCPG-UHFFFAOYSA-N thioanisole Chemical compound CSC1=CC=CC=C1 HNKJADCVZUBCPG-UHFFFAOYSA-N 0.000 abstract 1
Classifications
-
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
- Y02P20/00—Technologies relating to chemical industry
- Y02P20/50—Improvements relating to the production of bulk chemicals
- Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups
Landscapes
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
Abstract
PURPOSE: To prepare the titled compound having low toxicity and long-acting effectivity, and useful as an analgesic, etc., economically in an industrial scale, by reacting a specific encephaline derivative with trifluoromethanesulfonic acid as an agent for eliminating the protecting group, and a specific thioether derivative.
CONSTITUTION: The objective compound of formula III (R1 is lower alkyl) is prepared by reacting an encephaline derivative of formula I (R2 is aralkyloxycarbonyl, or alkoxycarbonyl; R3 is lower alkyl) with trifluoromethanesulfonic acid as an agent for eliminating the protecting group and a thioether derivative of formula II (R4 is lower alkyl), e.g. thioanisole, etc., in trifluoroacetic acid at -20W+50°C.
USE: The compound has agonist-activating activity to opiate-receptor, and useful as an analgesic, a narcotic antagonist, and an antidiarrhetic.
COPYRIGHT: (C)1981,JPO&Japio
Priority Applications (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP11219179A JPS5636441A (en) | 1979-08-31 | 1979-08-31 | Preparation of encephaline derivative |
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP11219179A JPS5636441A (en) | 1979-08-31 | 1979-08-31 | Preparation of encephaline derivative |
Publications (2)
Publication Number | Publication Date |
---|---|
JPS5636441A true JPS5636441A (en) | 1981-04-09 |
JPS6225160B2 JPS6225160B2 (en) | 1987-06-01 |
Family
ID=14580530
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP11219179A Granted JPS5636441A (en) | 1979-08-31 | 1979-08-31 | Preparation of encephaline derivative |
Country Status (1)
Country | Link |
---|---|
JP (1) | JPS5636441A (en) |
-
1979
- 1979-08-31 JP JP11219179A patent/JPS5636441A/en active Granted
Also Published As
Publication number | Publication date |
---|---|
JPS6225160B2 (en) | 1987-06-01 |
Similar Documents
Publication | Publication Date | Title |
---|---|---|
ES8204739A1 (en) | their starting compounds and their preparation. | |
FI891176A (en) | PEPTIDFOERENINGAR, FOERFARANDE FOER DERAS FRAMSTAELLNING OCH DESSA INNEHAOLLANDE PHARMACEUTISKA BLANDNINGAR. | |
DE68925223D1 (en) | 3-alkenyl-1-azabicyclo (3.2.0) hept-2-en-2-carboxylic acid compounds | |
ES2057016T3 (en) | ACID COMPOUNDS 3-PIRROLIDINYLTIO-1-AZABICICLO (3.2.0) HEPT-2-ENO-2-CARBOXILICO. | |
ZA81978B (en) | Substituted imidazole derivatives and their preparation and use | |
ATE50575T1 (en) | 2-OXIMINO-2-AMINOTHIAZOLYLACETIC ACID DERIVATIVES AND PROCESS FOR THEIR PRODUCTION. | |
ES8704153A1 (en) | Pyrimidine derivatives, processes for preparation thereof and composition of the same. | |
JPS5636441A (en) | Preparation of encephaline derivative | |
JPS5488242A (en) | Novel derivative of fortimicin b and its preparation | |
JPS5716855A (en) | 4-guanidinomethylcyclohexanecarboxylic acid ester and its preparation | |
IE810396L (en) | SALTS OF 4'-(9-ACRIDINYLAMINO)-METHANESULPHONE-m-ANISIDIDE | |
ES435274A1 (en) | Substituted benzamides | |
JPS5721400A (en) | Novel fortimicin derivative | |
JPS5479227A (en) | Glucosamine derivative and its preparation | |
JPS55143993A (en) | Azetidinone derivative and its preparation | |
JPS5610150A (en) | Preparation of nitrotoluene derivative | |
ES8101591A1 (en) | A procedure for the preparation of cefalosporine analogues. (Machine-translation by Google Translate, not legally binding) | |
JPS5626855A (en) | Enkephalin derivative and its preparation | |
ES8300709A1 (en) | Heterocyclic compounds, compositions thereof, their preparation and use. | |
JPS643189A (en) | Novel damavaricin fc carbamate derivative | |
JPS5683410A (en) | Plant growth regulator | |
JPS55104266A (en) | Novel pyridone derivative | |
JPS5634688A (en) | Preparation of cephapirin | |
ES8503004A1 (en) | Penicillin derivatives. | |
ES8305307A1 (en) | Peptide, process for preparation thereof and use thereof. |