329977-73-3

Upstream product

• 84163-13-3 6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole hydrochloride 
• 109-70-6 1.3-chlorobromopropane 
• 84163-77-9 6-fluoro-3-(4-piperidinyl)benzo[d]isoxazole 
• 632-02-0 3-chloropropyl p-toluenesulfonate 
• 150332-87-9 6-fluoro-3-[1-(3-hydroxypropyl)-4-piperidinyl]-1,2-benzisoxazole 

Downstream Products

• 133454-47-4 iloperidone 

Relevant academic research and scientific papers

Discovery of a new class of multi-target heterocycle piperidine derivatives as potential antipsychotics with pro-cognitive effect

A series of benzoisoxazoleylpiperidine derivatives were synthesized by using the multi-target strategies and their potent affinities for dopamine (DA), serotonin (5-HT) and human histamine H3 receptors have been evaluated. Of these compounds, t

Discovery of aryl-piperidine derivatives as potential antipsychotic agents using molecular hybridization strategy

Schizophrenia is a chronic, disabling mental disorder that affects about one percent of world's population. Drugs acting on multiple targets have been demonstrated to provide superior efficacy in schizophrenia than agents acting on single target. In this study, based on FW01, a selective potent 5-HT1A receptor agonist discovered via dynamic pharmacophore-based virtual screening, molecular hybridization strategy was employed to optimize its in vitro activity over D2 and 5-HT2A receptors. The optimized compound 9f was found to show dual potent D2 and 5-HT2A receptors antagonistic activity. In addition, compound 9f showed good in vivo metabolic stability with t1/2 of 2 h in ICR mice and good capability to penetrate the blood-brain barrier with Kp value of 4.03. These results demonstrated that the dual D2 and 5-HT1A receptor antagonist 9f could serve as a promising lead compound to discover potent antipsychotic agents.

Development and Kilogram-Scale Synthesis of a D2/5-HT2A Receptor Dual Antagonist (±)-SIPI 6360

The kilogram-scale synthesis of a D2/5-HT2A receptor dual antagonist (±)-SIPI 6360 was developed as an alternative treatment for schizophrenia. Specifically, three conditions were modified and optimized, including the Vilsmeier condi

Flow Synthesis in Hot Water: Synthesis of the Atypical Antipsychotic Iloperidone

Inductively heated steel reactors continuously perform organic transformations in water under high temperature conditions, utilizing the unique physiochemical properties of water at subcritical conditions. We demonstrated the power of this set-up in the continuous synthesis of the atypical antipsychotic drug iloperidone, in which we performed four out of five steps under aqueous conditions.

PROCESS FOR THE PREPARATION OF ILOPERIDONE

A process for the preparation of crystalline 1-[4-[3-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]propoxy]-3-methoxyphenyl]-ethanone (Iloperidone), which comprises the reaction between 3-[1-(3-chloropropyl)-4-piperidinyl]-6-fluoro-1,2-benzisoxazole and 3-methoxy-4-hydroxy-acetophenone.