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合成 1,3-二氟苯(Ⅰ)与1-乙酰哌啶-4-羰基氯(Ⅱ)在AlCl_3存在下在二氯甲烷中进行付-克缩合反应得Ⅲ,将Ⅲ在6NHCl中回流水解得Ⅳ,其与羟胺在乙醇中回流得肟(Ⅴ),其在沸水中用KOH环合得Ⅵ。最后,在溶于热DMF的K_2CO_3和KI的作用下,Ⅵ与Ⅶ缩合得本品。药理作用本品和ritanserin一样,在有关的5-羟色胺S_2的所有试验中均显示活性作用,且所用剂量较低(外周拮抗作用0.0011mg/kg,中枢拮抗作用0.014mg/kg)。在有关多巴胺-D_2的试验中,本品与氟哌啶醇一样,在初始0.016mg/kg剂量时即显示活性。而对于一些中枢神经系统控制的功能,如强直性昏厥的诱发则本品作用相对较小。用狗作定
Synthesis of 1,3-difluorobenzene (Ⅰ) with 1-acetylpiperidine-4-carbonyl chloride (Ⅱ) in the presence of AlCl_3 in methylene chloride was carried out in the reaction of Ⅲ-Ⅲ, Ⅲ in 6NHCl reflux hydrolysis To IV, it is refluxed with hydroxylamine in ethanol to give the oxime (V) which is cyclized with KOH in boiling water to afford VI. Finally, under the action of K 2 CO 3 and KI dissolved in hot DMF, VI and VII are condensed to obtain the product. Pharmacological effects This product, like ritanserin, shows an active effect in all relevant tests of serotonin S 2 with a lower dose (peripheral antagonism 0.0011 mg / kg, central antagonism 0.014 mg / kg). In the test for dopamine-D 2, the product showed the same activity as haloperidol at the initial dose of 0.016 mg / kg. For some functions of the central nervous system control, such as the induction of catalepsy is the role of this product is relatively small. Set with a dog