Mazapertine Synthesis
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Mazapertine Synthesis
Mazapertine (RWJ-37796) is an antipsychotic agent that was developed by Johnson & Johnson but never marketed. It exerts its pharmacological effect through affinity for dopamine D2, serotonin 5-HT1A, and α1-adrenergic receptors. Mazapertine is safe and well tolerated when administered orally. Analogs of mazapertine with conformational restriction have been prepared and have greater affinity for the 5-HT1A receptor. Synthesis Alkylation of 2-Nitrophenol Nitrophenols are compounds of the formula HOC6H5−x(NO2)x. The conjugate bases are called nitrophenolates. Nitrophenols are more acidic than phenol itself. Mono-nitrophenols with the formula HOC6H4NO2. Three isomeric nitrophenols exist: ... 8-75-5(1) with isopropyl bromide gives 2-isopropoxynitrobenzene 8753-50-3(2). Catalytic hydrogenation of nitro group gives 2-isopropoxyaniline 9026-74-2(3). Intermolecular ring formation of this aniline with nornitrogen mustard 34-22-5yields 1-(2-isopropoxyphenyl)piper ...
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Antipsychotic
Antipsychotics, also known as neuroleptics, are a class of Psychiatric medication, psychotropic medication primarily used to manage psychosis (including delusions, hallucinations, paranoia or disordered thought), principally in schizophrenia but also in a range of other psychotic disorders. They are also the mainstay together with mood stabilizers in the treatment of bipolar disorder. Prior research has shown that use of any antipsychotic is associated with smaller brain tissue volumes, including white matter reduction and that this brain shrinkage is dose dependent and time dependent. A more recent controlled trial suggests that second generation antipsychotics combined with intensive psychosocial therapy may potentially prevent pallidal brain volume loss in first episode psychosis. The use of antipsychotics may result in many unwanted side effects such as Extrapyramidal symptoms, involuntary movement disorders, gynecomastia, impotence, weight gain and metabolic syndrome. ...
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