92821-83-5Relevant articles and documents
NBS-mediated synthesis of β-keto sulfones from benzyl alcohols and sodium arenesulfinates
Muneeswara, Madithedu,Sundaravelu, Nallappan,Sekar, Govindasamy
, p. 3479 - 3484 (2019/05/21)
An efficient synthetic route towards the synthesis of β-keto sulfones has been developed from secondary benzyl alcohols using N-bromosuccinimide (NBS). The present protocol utilizes NBS as oxidant as well as brominating agent, readily accessible benzyl alcohols and sodium arenesulfinates as the sulfonylating reagent under mild conditions. The control experiments revealed that the reaction proceeds via oxidation of alcohol to ketone, α-bromination of ketone and nucleophilic substitution by sodium arenesulfinate. Furthermore, the efficiency of the methodology was tested with a gram scale reaction and also shown the synthetic utility.
Synthesis and antidepressant activity of arylalkanol-piperidine derivatives as triple reuptake inhibitors
Zheng, Yong-Yong,Guo, Lin,Zhen, Xue-Chu,Li, Jian-Qi
, p. 123 - 136 (2012/09/08)
A series of arylalkanol-piperidine derivatives was synthesized, and their triple reuptake inhibition and in vivo activities have been evaluated. Among them, compounds 2a, 2j, 2k, 2m and 2n exhibited high potency for 5-HT, NA and DA transporters. Optimized compounds 2j and 2m showed significant reduction of immobility time compared to that of vehicle in the mouse tail suspension test (TST) test at doses ranging from 10 to 50 mg/kg po, and were not generally motor stimulants at 50 mg/kg dose. In addition, compounds 2j and 2m displayed desirable pharmacokinetic properties in SD rats.
3,8-DIAZA-BICYCLO[4.2.0]OCT-8-YL AMIDES
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Page/Page column 62, (2012/07/13)
The present invention relates to 3,8-diaza-bicyclo[4.2.0]oct-8-yl amide derivatives of formula (I) Formula (I) wherein the relative configuration of the diazabicyclooctane moiety is cis; and wherein Ar1, and Ar 2 are as described in the description, to their preparation, to pharmaceutically acceptable salts thereof, and to their use as pharmaceuticals, to pharmaceutical compositions containing one or more compounds of formula (I), and especially to their use as orexin receptor antagonists.