摘要:
An improved method for preparing opipramol (I) is disclosed, wherein iminostilbene (II) is reacted with 1-bromo-3-chloropropane in the presence of a weak base selected from a hydrogen phosphate salt and an acetate salt and in the presence of a phase transfer agent to produce N-(3-halopropyl)iminostilbene (III), which is mixture of N-(3-chloropropyl)iminostilbene and N-(3-bromopropyl)iminostilbene, and then N-(3-halopropyl)iminostilbene is reacted with N-(2-hydroxyethyl)piperazine to form opipramol, as shown in the following equations, where X is chlorine or bromine. ##STR1##
摘要:
A tricyclic compound represented by the following formula (I): ##STR1## wherein R.sup.1 represents hydrogen, halogen or lower alkyl; A represents cyano, carboxyl, tetrazolyl, cyano-substituted phenyl, carboxyl-substituted phenyl or tetrazolyl-substituted phenyl; V represents --(CH.sub.2).sub.m -- wherein m is an integer of 0 to 2; W represents ##STR2## and Q.sup.1 --Q.sup.2 --Q.sup.3 --Q.sup.4 represents N.dbd.CH--CH.dbd.CH, CH.dbd.CH--CH.dbd.CH or CH.sub.2 --CH.sub.2 --CH.sub.2 --CH.sub.2, ##STR3## and Q represents N or CH; X.sup.1 --X.sup.2 --X.sup.3 represents CH.dbd.CH--CH.dbd.CH, S--CH.dbd.CH or CH.dbd.CH--S; Y represents CH.sub.2 CH.sub.2 ; and Z.sup.1 --Z.sup.2 represents N--(CH.sub.2).sub.n -- wherein n is an integer of 1 to 3 or a pharmaceutically acceptable salt thereof.
摘要:
Iminodibenzyl derivatives of the formula: ##SPC1##Wherein R and R.sup.1 each represent hydrogen, halogen, amino, sulfamoyl, lower alkyl, lower alkoxy or lower alkanoyl, provided that R and R.sup.1 can not both be hydrogen and when R and R.sup.1 are the same, they are located at positions asymmetric to each other, are produced in high purity and yield by a series of reactions which proceed through novel 2,2'-dinitrostilbene or 2,2'-diaminostilbene and 2,2'-diaminodibenzyl derivatives. The reaction sequence involves condensation, reduction and ring-closure reactions to give asymmetric as well as symmetric iminodibenzyl derivatives. The resulting iminodibenzyl derivatives may be converted to useful pharmaceutical compounds having anti-depressant, analgesic or anti-allergic properties.
摘要:
Preparation and the antiarrhythmic and antimicrobial properties of 5-alkyl-10-(aminocarbonyl/aminomethyl/cyano)-10,11-dihydro-5H-dibenz[b,f]azepine-10-alkanamines and equivalent salts are disclosed.
摘要:
This invention relates to tricyclic compounds bearing on the nitrogen atom of the medium ring an 3-amino 2-hydroxy propylamino carbonyl side chain and their physiologically compatible acid addition salts. This invention also relates to a process for making the same which includes the steps of condensing a tricyclic carbamic acid or one of its functional derivative with a 1,3-diamino 2-hydroxy propane derivative. The compounds of the invention have therapeutical utility namely in the cardiovascular field as antiarrythmic agents.
摘要:
A new process for the production of 10,11-dimethyl-5H-dibenz(b, f)azepines and 5,10,11-trimethyl-5H-dibenz(b,f)azepines as well as their 2- or 3- substituted derivatives comprises the following reaction steps: Condensation of a 9-methyl acridine with acetaldehyde, reduction of the obtained ketone to the corresponding secondary alcohol, followed by WAGNER-MEERWEIN rearrangement to the corresponding 10,11-dimethyl-5H-dibenz(b,f)azepine; illustrative embodiments are 10,11-dimethyl-5H-dibenz(b,f)azepine and 3-trifluoromethyl10,11-dimethyl-5H-dibenz(b,f)azepine.
摘要:
COMPOUNDS OF THE CLASS OF 1,2,3,8-TETRAHYDRO-DIBENZO (B,F)PYRROLO(3,4-D)JAZEPINES AND PHARMACEUITALLY ACCEPTABLE ACID ADDITION SALTS THEREOF HAVE A DEPRESSANT EFFECT ON THE CENTRAL NERVOUS SYSTEM; THEY CAN BE PREPARED FROM N-SUBSTITUTED 10,11-BIS-BROMOMETHYL-5HDIBENZ (B,F)AZEPINES AND A PRIMARY AMINE; THE COMPOUNDS ARE ACTIVE INGREDIENTS OF PHARMACEUTICAL COMPOSITIONS; AN ILLUSTRATIVE EMBODIMENT IS 2-ETHYL-1,2,3,9-TETRAHYDRODIBENZO(3,4-D)JAZEPINE.