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87760-53-0

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An efficient synthesis of buspirone and its analogues
-
Cybulski,Chilmonczyk,Szelejewski,Wojtasiewizc,Wrobel
p. 313 - 315
(2007/10/02)

Synthesis and anxiolytic activity of N-substituted cyclic imides (1R*,2S*3R*,4S*)-N-[4-[4-(2-pyrimidinyl)-1-piperazinyl]butyl]-2,3-b icyclo[2.2.1]heptanedicarboxime (Tandospirone) and related compounds
A series of cyclic imides bearing a ω-(4-aryl and 4-heteroaryl-1-piperazinyl)alkyl moieties was synthesized and tested in vivo for anxiolytic activity. The in vitro binding affinities of these compounds were also examined for 5-HT(1A) receptor sites. Structure-activity relationships within these series are discussed. One of these compounds, (1R*,2S*,3R*,4S*)-N-[4-[4-(2-pyrimidinyl)-1-piperazinyl]butyl]-2,3- bicyclo[2.2.1]heptanedicarboximide (1: tandospirone), was found to be equipotent with buspirone in its anxiolytic activity and more anxio-selective than buspirone and diazepam. Tandospirone (1) is currently undergoing clinical evaluation as a selective anxiolytic agent.
Ishizumi,Kojima,Antoku
p. 2288 - 2300
(2007/10/02)

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112457-95-1
tandospirone citrate

Chemical Properties

Melting Point: 112-113.5°
Boiling Point: 613.9 °C at 760 mmHg
Flash Point:325.1 °C
Density: 1.239g/cm³
Solubility:DMSO: soluble38mg/mL
Storage Temp.:Store at +4°C
Vapor Pressure: 5.23E-15mmHg at 25°C
Refractive Index: 1.589
PKA: 7.71±0.10(Predicted)
PSA: 69.64000
LogP: 1.35070

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