依匹哌唑合成路线图解
摘要
<正>精神分裂症及重度抑郁症(major depressive disorder,MDD)是两种最常见的严重精神类疾病,其致病机制不明,是可致残的脑部疾病,在世界范围内约有1%的人受其影响~[1]。另外,MDD可导致自杀,据世界卫生组织(WHO)统计,每年大约有100万人因此失去生命~[2]。随着社会压力的增大,精神分裂症的发病率不断上升,我国的患者也呈上升趋势。依匹哌唑(brexpiprazole)的中文化学名称:7-
This paper systematically reviewed the recent advance in the research and development of brexpiprazole and its intermediates7-hydroxyquinoline-2(1H)-one.This reviewsummarized and discussed rawmaterials,methods of brexpiprazole and 7-hydroxyquinoline-(1H)-2-one in organic synthesis and also gave its outlook in the future.
This paper systematically reviewed the recent advance in the research and development of brexpiprazole and its intermediates7-hydroxyquinoline-2(1H)-one.This reviewsummarized and discussed rawmaterials,methods of brexpiprazole and 7-hydroxyquinoline-(1H)-2-one in organic synthesis and also gave its outlook in the future.
引文
[1]LI Wen-jin,JI Wei-dong,LI Zhi-qiang,et al.Genetic association of ACSM1 variation w ith schizophrenia and major depressive disorder in the Han Chinese population[J].Am J M ed Genet B.Neuropsychiatr Genet,2015,168(B):144-149.
[2]徐磊,封宇飞.5-羟色胺-多巴胺受体部分激动剂依匹哌唑的药理作用及临床评价[J].中国新药杂志,2016,25(5):481-483.
[3]US FDA.FDA approves new drug to treat schizophrenia and as an add on an antidepressant to treat major depressive disorder[EB/OL].[2015-07-13].http://w w w.fda.gov/new sevents/new sroom/pressannouncement/ucm454647.htm.
[4]RICHELSON E.Multi-modality:a new approach for the treatment of major depressive disorder[J].Int J Neuropsychopharmacology,2013,30(16):1-10.
[5]吴之波,陈国良.依匹哌唑[J].中国药物化学杂志,2015,25(6):494.
[6]XIE Sai-sai,WANG Xiao-bing,JIANG Neng,et al.M ulti-targettacrine-coumarin hybrids:cholinesterase and monoamine oxidase B inhibition properties against Alzheimer's disease[J].Eur J M ed Chem,2015,95(3):153-165.
[7]ABD EI-AAL R M,KORAIERM A I M.Synthesis,absorption spectra studies and biolodical activity of some novel conjugate dyes[J].J Chin Chem Soc,2000,47(2):389-395.
[8]SHI Zhi-hao,LI Nian-guang,SHI Qian-ping,et al.Synthesis and structure:activity relationship analysis of caffeic acid amides as selective matrix metalloproteinase inhibitions[J].Bioorg M ed Chem Lett,2013,23(15):1206-1211
[9]EMMERSON J,PHILIP J.Triazolo-pyrazine derivatives useful in the treatment of disorders of the central nervous system:WO,2014085284[P].2014-06-05.
[10]赵爱明,倪秋洋.依匹哌唑中间体7-羟基喹啉-(1H)-2-酮的合成[J].精细石油化工,2017,34(2):55-58.
[11]CHEN Ye-long,WANG Tai-chi,FANG Kuo-chang,et al.Synthesis of certain quinolin-2(1H)-oneα-methylene-γ-butyeolactones as potential antiplatelet agents[J].Heterocycles,1999,50(1):453-462.
[12]WU Chun-hui,CHEN Wei-ming,JIANG De-hui,et al.An improved synthesis of 4-(1-piperazinyl)benzo[b]thiophenedihydrochloride[J].Org Process Res Dev,2015,19(4):555-558.
[13]王雪根,何凌云,余洋,等.一种依匹哌唑的制备方法:中国,105461704A[P].2016-04-06.
[14]KOICHI S,NAOTO U,MASAHIRO S,et al.Method for producing benzo[b]hiophene compound:US,20140187782[P].2014-07-03.
[15]徐奎,陶俊钰,刘经星.一种依匹哌唑新的制备方法:中国,105399736A[P].2016-03-16.
[16]张耀春,左小勇,张华娇,等.一种依匹哌唑的制备方法:中国,104829602A[P].2015-08-12.
[17]彭锦安,周革文.一种依匹哌唑的制备方法:中国,105461703A[P].2016-04-06.
[18]叶天健,陆修伟,郁光亮,等.一种依匹哌唑制备方法及其中间体和中间体的制备方法:中国,105541819A[P].2016-05-04.
[19]LEE Chia-Ying,HUANG Shu-ting,WANG HsinChi,et al.Processes for preparing brexpiprazole:WO,2017078621[P].2017-05-11.
[20]程刚.一种依匹哌唑的制备方法:中国,105175401A[P].2015-12-23.
[2]徐磊,封宇飞.5-羟色胺-多巴胺受体部分激动剂依匹哌唑的药理作用及临床评价[J].中国新药杂志,2016,25(5):481-483.
[3]US FDA.FDA approves new drug to treat schizophrenia and as an add on an antidepressant to treat major depressive disorder[EB/OL].[2015-07-13].http://w w w.fda.gov/new sevents/new sroom/pressannouncement/ucm454647.htm.
[4]RICHELSON E.Multi-modality:a new approach for the treatment of major depressive disorder[J].Int J Neuropsychopharmacology,2013,30(16):1-10.
[5]吴之波,陈国良.依匹哌唑[J].中国药物化学杂志,2015,25(6):494.
[6]XIE Sai-sai,WANG Xiao-bing,JIANG Neng,et al.M ulti-targettacrine-coumarin hybrids:cholinesterase and monoamine oxidase B inhibition properties against Alzheimer's disease[J].Eur J M ed Chem,2015,95(3):153-165.
[7]ABD EI-AAL R M,KORAIERM A I M.Synthesis,absorption spectra studies and biolodical activity of some novel conjugate dyes[J].J Chin Chem Soc,2000,47(2):389-395.
[8]SHI Zhi-hao,LI Nian-guang,SHI Qian-ping,et al.Synthesis and structure:activity relationship analysis of caffeic acid amides as selective matrix metalloproteinase inhibitions[J].Bioorg M ed Chem Lett,2013,23(15):1206-1211
[9]EMMERSON J,PHILIP J.Triazolo-pyrazine derivatives useful in the treatment of disorders of the central nervous system:WO,2014085284[P].2014-06-05.
[10]赵爱明,倪秋洋.依匹哌唑中间体7-羟基喹啉-(1H)-2-酮的合成[J].精细石油化工,2017,34(2):55-58.
[11]CHEN Ye-long,WANG Tai-chi,FANG Kuo-chang,et al.Synthesis of certain quinolin-2(1H)-oneα-methylene-γ-butyeolactones as potential antiplatelet agents[J].Heterocycles,1999,50(1):453-462.
[12]WU Chun-hui,CHEN Wei-ming,JIANG De-hui,et al.An improved synthesis of 4-(1-piperazinyl)benzo[b]thiophenedihydrochloride[J].Org Process Res Dev,2015,19(4):555-558.
[13]王雪根,何凌云,余洋,等.一种依匹哌唑的制备方法:中国,105461704A[P].2016-04-06.
[14]KOICHI S,NAOTO U,MASAHIRO S,et al.Method for producing benzo[b]hiophene compound:US,20140187782[P].2014-07-03.
[15]徐奎,陶俊钰,刘经星.一种依匹哌唑新的制备方法:中国,105399736A[P].2016-03-16.
[16]张耀春,左小勇,张华娇,等.一种依匹哌唑的制备方法:中国,104829602A[P].2015-08-12.
[17]彭锦安,周革文.一种依匹哌唑的制备方法:中国,105461703A[P].2016-04-06.
[18]叶天健,陆修伟,郁光亮,等.一种依匹哌唑制备方法及其中间体和中间体的制备方法:中国,105541819A[P].2016-05-04.
[19]LEE Chia-Ying,HUANG Shu-ting,WANG HsinChi,et al.Processes for preparing brexpiprazole:WO,2017078621[P].2017-05-11.
[20]程刚.一种依匹哌唑的制备方法:中国,105175401A[P].2015-12-23.