73438-28-5Relevant academic research and scientific papers
Synthesis and in vitro pharmacological evaluation of novel 2-hydroxypropyl-4-arylpiperazine derivatives as serotoninergic ligands
Fiorino, Ferdinando,Magli, Elisa,Severino, Beatrice,Corvino, Angela,Ciano, Antonio,Perissutti, Elisa,Frecentese, Francesco,Massarelli, Paola,Nencini, Cristina,Santagada, Vincenzo,Caliendo, Giuseppe
, p. 698 - 706 (2016/03/01)
This paper reports the synthesis of new norbornene and exo-N-hydroxy-7-oxabicyclo[2.2.1]hept-5-ene-2,3-dicarboximide derivatives and their binding to the 5-HT1A, 5-HT2A, and 5-HT2C receptors, in order to identify selective
New chemical and chemo-enzymatic routes for the synthesis of (RS)- and (S)-enciprazine
Banoth, Linga,Narayan, Thete Karuna,Banerjee, Uttam C.
, p. 1272 - 1278 (2012/11/07)
The chemo-enzymatic synthesis of racemic and enantiopure (RS)- and (S)-enciprazine 1, a non-benzodiazepine anxiolytic drug, is described herein. The synthesis started from 1-(2-methoxyphenyl) piperazine 3, which was treated with 2-(chloromethyl) oxirane (RS)-4 using lithium bromide to afford a racemic alcohol, 1-chloro-3-(4-(2-methoxyphenyl) piperazin-1-yl) propan-2-ol (RS)-6 in 85% yield. Intermediate (S)-6 was synthesized from racemic alcohol (RS)-6 using Candida rugosa lipase (CRL) with vinyl acetate as the acyl donor. Various reaction parameters such as temperature, time, substrate, enzyme concentration, and the effect of the reaction medium on the conversion and enantiomeric excess for the transesterification of (RS)-6 by CRL were optimized. It was observed that 10 mM of (RS)-6, 50 mg/mL of CRL in 4.0 mL of toluene with vinyl acetate (5.4 mmol) as acyl donor at 30 °C gave good conversion (C = 49.4%) and enantiomeric excess (eeP = 98.4% and eeS = 96%) after 9 h of reaction. Compound (S)-6 is a key intermediate for the synthesis of enantiopure (S)-1. The (RS)- and (S)-enciprazine drug 1 was synthesized by treating (RS)- and (S)-6 with 3,4,5-trimethoxyphenol 5 using MeCN as a solvent and K2CO3 as a base.
Investigations on the synthesis and pharmacological properties of 4-alkoxy-2-[2-hydroxy-3-(4-aryl-1-piperazinyl)propyl]-6-methyl-1H-pyrrolo [3,4-c]pyridine-1,3(2H)-diones
Sladowska, Helena,Filipek, Barbara,Szkatula, Dominika,Sabiniarz, Aleksandra,Kardasz, Malgorzata,Potoczek, Joanna,Sieklucka-Dziuba, Maria,Rajtar, Grazyna,Kleinrok, Zdzislaw,Lis, Tadeusz
, p. 897 - 908 (2007/10/03)
Synthesis of 2-[2-hydroxy-3-(4-aryl-1-piperazinyl)propyl] derivatives of 4-alkoxy-6-methyl-1H-pyrrolo[3,4-c]pyridine-1,3(2H)-diones (8-12) is described. The chlorides used in the above synthesis can exist in two isomeric forms: chain (18-20) and cyclic (19a, 20a). The compounds 8-12 exhibited potent analgesic activity which was superior than that of acetylsalicylic acid in two different tests. Most of the investigated imides suppressed significantly spontaneous locomotor activity in mice.
6-substituted purinyl piperazine derivatives
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, (2008/06/13)
Novel 6-substituted purinyl piperazine derivatives are described. The novel derivatives are useful as cardiotonic agents and antiarrhythmic agents.
