CAS: 39577-43-0; 1-(3-Chlorophenyl)-4-(3-Chloropropyl)Piperazine

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CAS号32229-98-4 1-Piperazinepro... | CAS号98-59-9 对甲苯磺酰氯(PTSC) | CAS号109-70-6 1-溴-3-氯丙烷 | CAS号6640-24-0 1-(3-氯苯基)哌嗪 | CAS号13078-15-4 1-(3-氯苯基)哌嗪盐酸盐 | CAS号6320-28-1 Piperazine,1-(3... | CAS号6323-10-0 1-(2-chlorophen...

盐酸曲唑酮杂质置于三苯基膦体系中,用 四氯化碳 用作溶剂,以70%的收率获得1-(3-氯苯基-4-氯丙基)哌嗪盐酦盐
参考文献:Synthesis Of 2-Phenylthiazolidine Derivatives As Cardiotonic Agents. Ii. 2-(Phenylpiperazinoalkoxyphenyl)Thiazolidine-3-Thiocarboxamides And The Corresponding Carboxamides.
标题:Synthesis Of 2-Phenylthiazolidine Derivatives As Cardiotonic Agents. Ii. 2-(Phenylpiperazinoalkoxyphenyl)Thiazolidine-3-Thiocarboxamides And The Corresponding Carboxamides.
摘要:大量2-(苯基哌嗪基烷氧苯基)噻唑烷-3-硫代羧酰胺及其相应羧酰胺(II)被合成并在麻醉犬中测试其强心活性.化合物ii通过羟基苯甲醛(III)及其中间体(iv,V和x)制备.通过改变结构参数来研究结构-活性关系(sar).将哌嗪基烷氧基团从邻位位置移至间位或对位导致活性显著下降.将硫代羧酰胺转变为羧酰胺基团导致活性显著增加.这种趋势在这一系列化合物中普遍存在,并构成与简单2-苯基噻唑烷系列sar的主要偏离.关于氨基烷氧链长度的影响,乙氧基衍生物通常比更高级的类似物更有效.在(硫代)羧酰胺基团中延长n-烷基通常导致活性下降.在合成的各种衍生物中,Ii15被发现其效力约为氨力农的一百倍,且作用时间较长.
Doi:10.1248/cpb.35.2394

专利信息

专利号:US-6084097-A
优先权日:1997-10-20
标题:Methods for preparing 1-[4-arylpiperazin-1-yl]-3-[2-oxopyrrolidin/piperidin-1-yl] propanes
发明人：SINHA NEELIMA; JAIN SANJAY; SAXENA ANIL KUMAR; ANAND NITYA; SAXENA RAM MOHAN; DUBEY MANGAL PRASAD; RAY MADHUR; PATNAIK GYANENDRA KUMAR
权利人:COUNCIL SCIENT IND RES
摘要:The invention relates to a process for the synthesis of 1-[4-Arylpiperazin-1-yl]-3-[2-oxopyrrolidin/piperidin-1-yl]propanes used as potential therapeutic agents for hypertension, ischemia, cardiovascular and other adrenergic receptors related disorders, having general formula 1 ##STR1## wherein Ar represents a phenyl ring substituted by the groups like halo, alkoxy, alkyl or heteroaryl, n=1 or n=2; a process of preparing said compounds and a method of treating hypertension, ischemia, cardiovascular and other adrenergic receptors related disorders.

专利号:EP-0913397-B1
优先权日:1997-10-22
标题:A proces for the synthesis of 1-(4-Arylpiperazine-1-y1)-3-(2-oxypyrrolidin/piperidin-1-yl)propanes as therapeutic agents for hypertension, ischemia, cardiovascular and other adrenergic receptors related disorders
发明人：SINHA NEELIMA; JAIN SANJAY; SAXENA ANIL KUMAR; ANAND NITYA; SAXENA RAM MOHAN; DUBEY MANGAL PRASAD; PATNAIK GYANENDRA KUMAR
权利人:COUNCIL SCIENT IND RES

专利号:DE-69736291-T2
优先权日:1997-10-22
标题:A process for the synthesis of 1- (4-arylpiperazin-1-yl) -3- (oxopyrrolidine / piperidin-1-yl) propanes as therapeutic agents in hypertension, ischemia, cardiovascular and other disorders associated with adrenergic receptors

专利号:US-4596884-A
优先权日:1983-11-30
标 题 :4-(2-phenoxyethyl)-1,2,4-triazolone process intermediates
发明人：MADDING GARY D
权利人:BRISTOL MYERS CO
摘要:An improved process for the preparation of 5-ethyl-4-(2-phenoxyethyl)-1,2,4-triazolone, a useful intermediate in the synthesis of antidepressant 1,2,4-triazolones typified by 2-[3-[4-(3-chlorophenyl)-1-piperazinyl]propyl]-5-ethyl-4-(2-phenoxethyl)-2H-1,2,4-triazol-3(4H)-one, also known as nefazodone. The improved process is shorter and higher in yield than the former process, and the starting materials are cheap and readily available.

专利号:EP-0913397-A1
优先权日:1997-10-22
标 题 :A proces for the synthesis of 1-(4-Arylpiperazine-1-y1)-3-(2-oxypyrrolidin/piperidin-1-y1) propanes as therapeutic agents for hypertension, ischemia, cardiovascular and other adrenergic receptors related disorders