74760-14-8Relevant academic research and scientific papers
A simple and efficient asymmetric synthesis of anxiolytic drug enciprazine
Narsaiah, A. Venkat,Nagaiah
experimental part, p. 2705 - 2707 (2010/10/18)
A straightforward and efficient asymmetric synthesis of (S)-1-[4-(2-methoxyphenyl)piperazin-1-yl]-3-(3,4,5-trimethoxyphenoxy) propan-2-ol is described. The key intermediate, (S)-2-[(3,4,5-trimethoxyphenoxy) methyl]oxirane, was obtained by a hydrolytic kinetic resolution method using the catalyst (R,R)-salen-cobalt(III) complex. Georg Thieme Verlag Stuttgart.
Chemistry and Pharmacology of the Non-Benzodiazepine Anxiolytic Enciprazine and Related Compounds
Engel, Juergen,Fleischhauer, Ilona,Jakovlev, Vladimir,Kleemann, Axel,Kutscher, Bernhard,et al.
, p. 2976 - 2981 (2007/10/02)
In the course of studies on tranquilizers, new non-benzodiazepine-like compounds were synthesized.These are 1-(3,4,5-trimethoxyphenoxy)-3-propan-2-ol (INN: enciprazine) and derivatives thereof which were screened pharmacologically in order to evaluate their central nervous system activity.Compounds with marked antiaggressive and anxiolytic properties but without dependence potential could be detected.Enciprazine was selected for clinical investigations.
Cardioselective aryloxy- and arylthio- hydroxypropylene-piperazinyl acetanilides which affect calcium entry
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, (2008/06/13)
Novel compounds of the general formula STR1 and the pharmaceutically acceptable esters and acid addition salts thereof, wherein: R1, R2, R3, R4 and R5 are each independently hydrogen, lower alkyl, lower alkoxy, cyano, trifluoromethyl, halo, lower alkylthio, lower alkyl sulfinyl, lower alkyl sulfonyl, N-optionally substituted alkylamido, except that when R1 is methyl, R4 is not methyl; or R2 and R3 together form --OCH2 O--; R6, R7, R8, R9 and R10 are each independently hydrogen, lower acyl, aminocarbonylmethyl, cyano, lower alkyl, lower alkoxy, trifluoromethyl, halo, lower alkylthio, lower alkyl sulfinyl, lower alkyl sulfonyl, di-lower alkyl amino; or R6 and R7 together form --CH=CH--CH=CH--; R7 and R8 together form --OCH2 O--; R11 and R12 are each independently hydrogen or lower alkyl; and W is oxygen or sulfur. These cardioselective compounds have calcium entry blockade properties and therefore are useful in therapy in the treatment of cardiovascular diseases, including arrhythmias, variant and exercise induced angina and myocardial infarction.
