摘要:
Compounds having a mercaptoethyl group are prepared by reacting an aqueous thiocyanate solution with ethylene oxide in the presence of an inert water immiscible organic solvent to form ethylene sulfide and then reacting the organic phase with a polar organic compound, preferably a secondary amine.
摘要:
There are produced 6-aza-3H-1,4-benzodiazepines and 6-aza-1,2-dihydro-3H-1,4-benzodiazepines of the formula ##STR1## where R.sub.1 is a halogen, R.sub.2 and R.sub.3 are hydrogen, halogen, trifluoromethyl, nitro, nitrile, hydroxy, lower alkyl, lower alkoxy, R.sub.4 is hydrogen, hydroxyl, hydroxyl acylated with a mono or dicarboxylic aid of 2 to 6 carbon atoms, lower alkoxy, lower alkyl, benzyl, lower aliphatic acyl, carboxy or carb-lower alkoxy, Z is nitrogen or NO, R.sub.5 is hydrogen, lower alkyl, lower alkyl substituted with cycloalkyl of 3 to 6 carbon atoms, lower alkenyl, cycloalkyl of 3 to 6 carbon atoms, lower hydroxyalkyl, benzyl, aliphatic acyl of 2 to 6 carbon atoms aminoalkyl of 2 to 7 carbon atoms, mono or di lower alkyl substituted aminoalkyl of 2 to 7 carbon atoms, lower alkyl substituted with 5 to 7 membered N-heterocyclic ring, containing 0 to 1 additional nitrogen or oxygen atoms, and A is oxygen, sulfur, .dbd.NR.sub.5, .dbd.NOR.sub.5, .dbd.NH--NHR.sub.5 or two hydrogen atoms and the --N(R.sub.5)--C--(.dbd.A)-- can also be in the tautomeric form --N.dbd.C(AR.sub.5) 13 and pharmacologically acceptable salts thereof. The compounds have spasmolytic, antiphlogistic and tranquilizer activity.
摘要:
Chloromethyl thiocyanate is prepared by reacting bromochloromethane with an alkali or alkaline earth thiocyanate or with ammonium thiocyanate in the presence of water and an onium salt as a catalyst.
摘要:
The calcium salts of mono-hydroxymethyl lysine and bis(hydroxymethyl) lysine are prepared by reacting lysine and formaldehyde in water containing calcium ions at a pH of at least 8 and at most 12.5. The compounds are useful as fodder for ruminants.
摘要:
Compounds are prepared having the formula: ##STR1## where R.sub.1 is alkyl of 1 to 6 carbon atoms or phenyl and R.sub.2 is hydrogen or halogen and tautomeric form and pharmacologically acceptable salts thereof. The compounds have sedative, psychosedative, anxiolytic and spasmolytic properties and in some cases antiphlogistic properties.
摘要:
There are produced 6-aza-3H-1,4-benzodiazepines and 6-aza-1,2-dihydro-3H-1,4-benzodiazepines of the formula: ##STR1## wherein R.sub.1 is the group --NR.sub.a R.sub.b or --NR.sub.a R.sub.b R.sub.c halide and R.sub.a and R.sub.b are the same or different and are hydrogen, alkyl groups of 1 to 6 carbon atoms, or alkyl groups of 1 to 6 carbon atoms substituted by hydroxy, phenyl or a carboxy group, and R.sub.c can be as defined for R.sub.a and R.sub.b except it cannot be hydrogen and wherein the group --NR.sub.a R.sub.b also can be a saturated closed 5, 6 or 7 membered ring which in a given case has a further oxygen atom or nitrogen atom or contains a nitrogen atom substituted with an alkyl group having 1 to 4 carbon atoms;R.sub.2 and R.sub.3 are the same or different and are hydrogen, halogen, trifluoromethyl, nitro, nitrile, hydroxy, lower alkyl or lower alkoxy;R.sub.4 is hydrogen;Z is a nitrogen atom or the NO group;R.sub.5 is hydrogen, lower alkyl, lower alkenyl, aminoalkyl of 2 to 4 carbon atoms, mono or di lower alkyl substituted aminoalkyl of 2 to 4 carbon atoms; andA is oxygen, and the --N(R.sub.5)--C--(=A)--can also be in the tautomeric form --N=C(AR.sub.5)--, pharmacologically acceptable salts and quaternary ammonium and alkyl ammonium compounds thereof. The compounds have pharmacodynamic properties including psychosedative and anxiolytic properties as well as antiphlogistic properties.
摘要:
There are prepared compounds of the formula: ##SPC1##Wherein:n is an integer from 1 to 4;R.sub.1 is alkyl of 1 to 6 carbon atoms, a hydroxy group, an amino group, an alkoxy group having 1 to 6 carbon atoms, a phenyl group or a phenyl group substituted with alkyl of 1 to 6 carbon atoms, an alkoxy group of 1 to 6 carbon atoms, trifluoromethyl, fluorine or chlorine;A is oxygen, sulfur, the imino group, or an alkylimino group having 1 to 6 carbon atoms, or when R.sub.1 is phenyl or substituted phenyl A also is two alkoxy groups having 1 to 6 carbon atoms or alkylenedioxy with 2 to 4 carbon atoms or --C(R.sub.1)=A is the cyano group;B is oxygen, sulfur, an imino group or an alkylimino group having 1 to 6 carbon atoms;R.sub.2 is hydrogen, a hydroxy group, an alkyl group with 1 to 6 carbon atoms, an alkoxy group with 1 to 6 carbon atoms, or the group --O(CH.sub.2).sub.n -- C(=A)--R.sub.1 ;N.sub.o is nitrogen or an N-oxide group; andR.sub.3 and R.sub.4 are the same or different and are hydrogen, chlorine, fluorine, the trifluoromethyl group, alkyl groups of 1 to 6 carbon atoms or alkoxy groups with 1 to 6 carbon atoms, the tautomeric forms thereof and pharmaceutically acceptable salts thereof. The compounds have psychosedative, anxiolytic, spasmolytic and antipsychotic activity.
摘要:
There are produced 6-aza-3H-1,4-benzodiazepines and 6-aza-1,2-dihydro-3H-1,4-benzodiazepines of the formula: ##SPC1##Wherein R.sub.1 is the group --NR.sub.a R.sub.b, --NR.sub.a R.sub.b R.sub.c or --NR.sub.a acyl and R.sub.a, R.sub.b and R.sub.c are the same or different and are hydrogen, alkyl groups of 1 to 6 carbon atoms, or alkyl groups of 1 to 6 carbon atoms substituted by hydroxy, an alkoxy group of 1 to 6 carbon atoms, a carboxy group, a nitrile group, a carbamide group, a carbalkoxy group with 1 to 6 carbon atoms in the alkoxy, a phenyl group or a halogen and acyl is an aliphatic acyl group with 2 to 6 carbon atoms and wherein the group --NR.sub.a R.sub.b also can be a saturated closed 5, 6 or 7 membered ring which in a given case has a further oxygen atom or nitrogen atom or contains a nitrogen atom substituted with an alkyl group having 1 to 4 carbon atoms;R.sub.2 and R.sub.3 are the same or different and are hydrogen, halogen, trifluoromethyl, nitro, nitrile, hydroxy, lower alkyl, lower alkoxy and R.sub.2 also can be --NR.sub.a R.sub.b, --NR.sub.a R.sub.b R.sub.c or the group --NR.sub.a acyl with the proviso that if R.sub.2 is --NR.sub.a R.sub.b, --NR.sub.a R.sub.b R.sub.c or --NR.sub.a acyl then R.sub.1 can be halogen;R.sub.4 is hydrogen, hydroxyl, hydroxyl acylated with a mono or dicarboxylic acid of 2 to 6 carbon atoms, a lower alkoxy group, a lower alkyl group, a benzyl group, lower aliphatic acyl, a carboxy group or a lower carbalkoxy group;Z is a nitrogen atom or the NO group;R.sub.5 is hydrogen, lower alkyl, lower alkyl substituted with cycloalkyl of 3 to 6 carbon atoms, lower alkenyl, cycloalkyl of 3 to 6 carbon atoms, lower hydryxoalkyl, benzyl, aliphatic acyl of 2 to 6 carbon atoms, aminoalkyl of 2 to 7 carbon atoms, mono or di lower alkyl substituted aminoalkyl of 2 to 7 carbon atoms, aminoalkyl of 2 to 7 carbon atoms substituted with a 5 to 7 membered heterocyclic ring including the amino nitrogen containing 0 to 1 additional nitrogen or oxygen atom; andA is oxygen, sulfur, =NR.sub.5, =NOR.sub.5, =NH--NHR.sub.5 or two hydrogen atoms, and the --N(R.sub.5)--C--(=A)-- can also be in the tautomeric form --N=C(AR.sub.5)--, pharmacologically acceptable salts and quaternary compounds thereof. The compounds have pharmacodynamic properties including psychosedative and anxiolytic properties as well as antiphlogistic properties.