摘要:
Novel bis basic esters of 9-substituted phenanthrene and related 9-oxa and 9-aza derivatives thereof, their preparation and use for the prevention and inhibition of viral infections are disclosed.
摘要:
Improved selectivity of desired vinylated aromatic compounds may be obtained when aromatic compounds are treated with an ethylenic compound in the presence of certain metallic catalysts by effecting the reaction in an acidic solvent medium, the dielectric constant of said solvent being less than 6.15.
Z IS A MEMBER SELECTED FOR THE GROUP CONSISTING OF
-OR4, -N(-R5)-R6
-CL,-BR, AND -OM; R, R2, R3, AND R5 ARE INDEPENDENTLY SELECTED FROM THE GROUP CONSISTING OF -H, LOWER ALKYL, PHENYL AND BENZYL, R6 IS SELECTED FROM THE GEOUP CONSISTING OF -H, LOWER ALKYL, PHEMYL, BENZYL, LOWER DIALKYLAMINOALKYL AND CYCLOALKYL OF 3 TO 10 CARBON ATOMS, AND WHEN TAKEN WITH R5 AND THE NITROGEN ATOM TO WHICH THEY ARE BONDED FORMS THE MORPHOLINO, PIPERIDINO AND PIPERAZINO GROUPS, AND M IS SELECTED FROM ALKALI METAL CATION AND -NH4, ARE IMMUNO-INFLAMMATORY AGENTS POSSESSING ANTIALLERGIC AND ANTIINFLAMMATORY ACTIVITY. THE COMPOUNDS OF THSI INVENTION ARE ALSO INTERMEDIATES FOR THE SYNTHESIS OF KNOWN CHROMONE AND COUMARIN DERIVATIVES.
WHEREIN: R1 IS A MEMBER SELECTED FROM THE GROUP CONSISTING OF HYDROGEN, LOWER ALKYL, LOWER ALKOXY, AND LOWER ALKYLTHIO; R2 IS A MEMBER SELECTED FROM THE GROUP CONSISTING OF HYDROGEN, LOWER ALKYL, LOWER ALKOXY, AND LOWER ALKYLTHIO; R6 IS A MEMBER SELECTED FROM THE GROUP CONSISTING OF HYDROGEN, LOWER ALKYL, LOWER ALKYLTHIO, LOWER AKLANOYLTHIO, AND HALO; R7 IS A MEMBER SELECTED FROM THE GROUP CONSISTING OF HYDROGEN, LOWER ALKYL, LOWER ALKYLTHIO, LOWER ALKANOYLTHIO, AND HALO; R11 IS A MEMBER SELECTED FROM THE GROUP CONSISTING OF HYDROGEN, HYDROXY AND LOWER ALKANOYLOXY; R16 IS A MEMBER SELECTED FROM THE GROUP CONSISTING OF HYDROGEN, LOWER ALKYL, HYDROXY, LOWER ALKOXY, LOWER ALKANOYLOXY, AND, WHEN THE 17B-SUBSTITUENT IS ACETYL OR SUBSTITUTED ACETYL, FLUORINE; Z IS A MEMBER SELECTED FROM THE GROUP CONSISTING OF CARBONYL, (17B-HYDROXY-17-A-LOWER ALKANOIC ACID LACTONE), AND
>C(-R17ALPHA)-R17BETA
R17B IS A MEMBER SELECTED FROM THE GROUP CONSISTING OF HYDROXY, LOWER ALKANOYLOXY, AND
Y-CH2-CO-
Y IS A MEMBER SELECTED FROM THE GROUP CONSISTING OF HYDROGEN, HALO, AND HYDROXY; R17A, WHEN R17B IS HYDROXY AND LOWER ALKANOYLOXY, IS A MEMBER SELECTED FROM THE GROUP CONSISTING OF HYDROGEN AND LOWER ALIPHATIC HYDROCARBYL, AND WHEN R17B IS
Y-CH2-CO-
IS A MEMBER SELECTED FROM THE GROUP CONSISTING OF HYDROGEN ALKYL, HYDROXY, LOWER ALKANOYLOXY, AND HALO; Q WHEN TAKEN ALONE, IS OXO; T1 WHEN TAKEN ALONE, IS A MEMBER SELECTED FROM THE GROUP CONSISTING OF ALKALI METAL OXY AND LOWER ALKOXY; AND T1 AND Q, WHEN TAKEN TOGETHER ARE NITROLO.
OR THE HYDROCHLORIC ACID ADDITION SALTS THEREOF, AND TO METHODS OF PREPARING SAME EITHER BY ACYLATING, IN THE PRESENCE OF ACID-BINDING AGENTS, IF DESIRED, COUMARIN DERIVATIVES HAVING THE FORMULA
WITH AN AMINE HAVING THE FORMULA RH, WHEREIN R IS SELECTED FROM SECONDARY FURFURYLAMINO AND SECONDARY TETRAHYDROFURFURLAMINO, WHICH IS BOUND VIA THE NITROGEN ATOM, R1 IS SELECTED FROM THE GROUP CONSISTING OF ALKYL RADICALS HAVING 1-4 CARBON ATOMS AND PHENYL, R2 IS SELECTED FROM THE GROUP CONSISTING OF 5,6-, 6,7-, AND 7,8POSITIONED ALKOXY GROUPS HAVING 1-4 CARBON ATOMS, R3 IS SELECTED FROM ALKOXY GROUPS HAVING 1-4 CARBON ATOMS, R4 IS SELECTED FROM THE GROUP CONSISTING OF CHLORINE AND BROMINE, R'' IS SELECTED FROM THE GROUP CONSISTING OF SECONDARY FURFURLAMINO AND SECONDARY TETRAHYDROFURFURYLAMINO, AND M IS SELECTED FROM THE GROUP CONSISTING OF 1, 2, AND 3.
摘要:
DI-HYDROXY PRODUCTS OF MONOHYDRIC PHENOL COMPOUNDS ARE PREPARED BY PERSULFATE OXIDATION IN THE PRESENCE OF EHTYLENEDIAMINETERTRAACETIC ACID AND AN OLEFINC FREE RADICAL TRAP.
摘要:
4-OXO-9-HYDROXY-7-(3-METHYL - 2 - OCTYL)-1,2,3,4-TETRAHYDROCYCLOPENTA(C)(1)BENZOPYRAN, USED AS AN INTERMEDIATE IN THE PREPARATION OF 1,2,3,4-TETRAHYDROCYCLOPENTA(C)(1)BENZOPYRANS AND 1,2,3,4,12,13-HEXAHYDROCYCLOPENTA(C)(1)BENZOPYRANS WHICH HAVE C.N.S. ACTIVITY.
摘要:
New 3-substituted-4-hydroxy-coumarins of the formula:
WHEREIN R1 represents a lower alkyl radical containing 1 to 3 carbon atoms and X represents chlorine, bromine or iodine; pharmaceutical compositions containing such compounds and a process for making the compounds are disclosed.
摘要:
THIS INVENTION RELATES TO PHENOL PHTHALEIN INDICATOR DYES CONTAINING AS THE RING-CLOSING MOIETY, A NAPHTHALIDE GROUP OR A CARBOXYPHTHALIDE GROUP POSSESSING A CARBOXY SUBSTITUENT IN EITHER THE 4- AND/OR 7-POSITION OF THE PHTHALIDE RING. IN A PREFERRED EMBODIMENT, THE PHENOL RADICALS ARE SUBSTITUTED WITH A HYDROGEN-BONDING GROUP ON A CARBON ATOM ADJACENT TO THE CARBON ATOM CONTAINING THE PHENOLIC -OH. THESE DYES, DUE TO THE NAPHTHALIDE OR CARBOXYPHTHALIDE RING-CLOSING MOIETY EXHIBIT IMPROVED STABILITY IN HIGHLY ALKALINE MEDIA AND WHEN SUBSTITUTED WITH HYDROGEN-BONDING GROUPS AS IN THE THE PREFERRED EMBODIMENT, POSSESS A RELATIVELY HIGH PKA AS WELL.
摘要:
3 - (BETA-DIALKYLAMINOETHYL) - 4-ALKYL-7-CARBOETHOXYMETHOXYCOUMARIN OF THE FORMULA:
3-(R2-N(-R3)-CH2-CH2-),4-R1,7-(C2H5-OOC-CH2-O-)-
2H-CHROMEN-2-ONE
IN WHICH R1, R2 AND R3 STAND FOR A LOWER ALKYL GROUP CONTAINING 1-3 CARBON ATOMS AND ITS HYDROHALIDES. THE ABOVE-MENTIONED COMPOUNDS PROVED TO BE DRUGS USED IN CASE OF CIRCULATORY SYSTEM DISEASES. THE SAID COMPOUNDS ARE PRODUCED IN THE REACTION OF RESORCINOL WITH A GAMMA-BUTYROLACTONE DERIVATIVE OF THE FORMULA:
3-(R1-CO-)TETRAHYDROFURAN-2-ONE
OR BY ADDITION OF A HYDROGEN HALIDE IN THE PRESENCE OF PHOSPHOROUS ACID (PIII) THEN THE THUS OBTAINED 3-(BETAHALOETHYL-4-ALKYL-7-HYDROXYCOUMARIN IS SUBJECTED TO REACTION WITH A HALOACETIC ACID ETHYL ESTER IN THE PRESENCE OF ALKALI METAL CARBONATE AND A CATALYTIC QUANTITY OF DIETHYLFORMAMIDE OR WATER AND POTASSIUM IODIDE. THE THUS OBTAINED 3-(BETA-HALOETHYL)-4-ALKYL-7-CARBOETHOXYMETHOXYCOUMARIN IS SUBJECTED TO REACTION WITH A DIALKYLAMINE AND THE THUS OBTAINED PRODUCT IS ISOLATED AS A COMPLEX COMPOUND WITH ZINC CHLORIDE AND IF NECESSARY CONVERTED TO THE HYDROHALIDE.