2-Chlorosulfenylbenzoyl Chloride置于ammonium Hydroxide,三氯氧磷体系中,用 二氯甲烷 作为反应溶剂,化学反应 4.5H,反应生成 3-氯-1,2-苯并异噻唑 参考文献:Synthesis And Biological Evaluation Of 1-(1,2-Benzisothiazol-3-yl)-And (1,2-Benzisoxazol-3-yl)Piperazine Derivatives As Potential Antipsychotic Agents 标题:Synthesis And Biological Evaluation Of 1-(1,2-Benzisothiazol-3-yl)-And (1,2-Benzisoxazol-3-yl)Piperazine Derivatives As Potential Antipsychotic Agents 摘要:Members Of The Series Of Title Compounds Were Tested For Potential Antipsychotic Activity In Relevant Receptor Binding Assays And Behavioral Screens. Structure-Activity Relationships Within The Series Are Discussed. Compound 24 (Bmy 13859-1),A (1,2-Benzisothiazol-3-yl)Piperazine Derivative,Was Selected For Further Study Because Of Its Potent And Selective Profile In Primary Cns Tests. It Was Active In The Sidman Avoidance Paradigm And Blocked Amphetamine-Induced Stereotyped Behavior In Dogs For Up To 7 H. The Compound'S Lack Of Typical Neuroleptic-Like Effects In The Rat Catalepsy Test And Its Failure To Produce Dopamine Receptor Supersensitivity Following Chronic Administration Indicate That It Should Not Cause The Movement Disorders Commonly Associated With Antipsychotic Therapy. Although 24 Has Potent Affinity For Dopaminergic Binding Sites,Its Even Greater Affinity For Serotonin Receptors Suggests That A Serotonergic Component May Be Relevant To Its Atypical Profile. Compound 24 Is Currently Undergoing Clinical Evaluation In Schizophrenic Patients. DOI:10.1021/jm00153A010
专利号:WO-2020240266-A1 优先权日:2019-05-31 标题:New endoperoxide compounds, process for obtaining them and uses thereof for control of perkinsiosis in bivalves 发明人:CRISTIANO MARIA; CABRAL LÃ?LIA; LEITE RICARDO; LEAL JOSÉ 权利人:CCMAR CENTRO DE CIENCIAS DO MAR UNIV DO ALGARVE; INST GULBENKIAN DE CIENCIA 摘要:The present invention relates to new endoperoxide compounds and compositions, and to a process for producing them for prophylaxis and control of perkinsiosis in bivalves. Endoperoxide compounds with biological activity against Perkinsus olseni include 13 trioxolanes and 9 tetraoxanes. Protozoan parasites of the genus Perkinsus are known to infect several species of marine molluscs worldwide, like oysters, abalones, clams, scallops, pearl oysters, cockles or mussels. The present invention also describes the synthesis of these compounds, in particular of new endoperoxide compounds of the tetraoxane family. Compositions comprising endoperoxide compounds are useful for prophylaxis and control of perkinsiosis in bivalves. Therefore, the present invention also relates to a method of controlling perkinsiosis in bivalves. The present invention is in the domain of aquaculture, medicine, pharmaceuticals and biochemistry.
专利号:RU-2090565-C1 优先权日:1991-02-27 标题 :Racemic or optically active perhydro-1h-pyrido-[1,2-a]-pyrazines or their pharmaceutically acceptable salts and method of their synthesis
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