Phthalides represent an important class of bioactive heterocycle extensively found in pharmaceuticals and natural products,their syntheses have attracted extensively attention.A water-promoted and rhodium-catalyzed[3+...Phthalides represent an important class of bioactive heterocycle extensively found in pharmaceuticals and natural products,their syntheses have attracted extensively attention.A water-promoted and rhodium-catalyzed[3+2]tandem cyclization of aromatic acids and acrylates has been developed in air and neat water free of any additives,which provides an environmentally benign approach for constructing phthalide motifs.Compared with previous literatures,this methodology features quite simple reaction conditions,simple operation and additive-free.Mechanistic studies indicate that apart from the many other well-known oxidations of Rh(I)by external oxidant,hydrogen transfer with the acrylate being a hydrogen acceptor is involved to regenerate the active Rh species,which is different from documented metal-catalyzed phthalides syntheses.The application of this protocol is further demonstrated by the green synthesis of biologically active isoochracinic acid in one step.展开更多
Transition-metal catalyzed cross-coupling is one of the basic strategies for the C-C bond formation.However,it is difficult to achieve satisfactory results when terminal alkynes with electron-withdrawing group such as...Transition-metal catalyzed cross-coupling is one of the basic strategies for the C-C bond formation.However,it is difficult to achieve satisfactory results when terminal alkynes with electron-withdrawing group such as propiolate esters are used.The reason behind this might be the easy polymerization of this type of alkynes in the presence of base.A tetrahydroxydiboron and copper sulfate co-promoted cross-coupling/cyclization of propiolate esters and o-iodobenzoic acid for the facile and efficient construction of phthalides is described.Preliminary mechanism study indicates that tetrahydroxydiboron can inhibit the polymerization of propiolate esters and increase the reaction rate.This method is characterized by high regio-and stereoselectivities,mild reaction conditions,short reaction time,broad substrate scope,and excellent functional group compatibility.展开更多
An efficient and facile method for the synthesis of 3-indolyl-substituted phthalides by Friedel-Crafts alkylation of indoles with 3-hydroxyisobenzofuran-1(3H)-one has been developed. Using only 2 mol-% TsOH·H2O a...An efficient and facile method for the synthesis of 3-indolyl-substituted phthalides by Friedel-Crafts alkylation of indoles with 3-hydroxyisobenzofuran-1(3H)-one has been developed. Using only 2 mol-% TsOH·H2O as the catalyst, various substituted indoles can react smoothly at room temperature to give the corresponding phthalides products in good to excellent yields (up to 96%).展开更多
目的探讨丁苯酞对大面积脑梗死预后的影响。方法选取201 1年2月~2013年12月期间,在哈励逊国际和平医院神经内科住院的大面积脑梗死患者92例作为研究对象,采用对照研究。将患者随机分为对照组(n=46)和治疗组(n=46)。对照组给予依达拉奉...目的探讨丁苯酞对大面积脑梗死预后的影响。方法选取201 1年2月~2013年12月期间,在哈励逊国际和平医院神经内科住院的大面积脑梗死患者92例作为研究对象,采用对照研究。将患者随机分为对照组(n=46)和治疗组(n=46)。对照组给予依达拉奉注射液静脉滴注,治疗组在此基础上给予丁苯酞胶囊联合治疗。2组患者均持续给药,疗程为2周。利用神经功能缺损程度评分(national institute of health stroke scale,NIHSS)^([1])评定2组患者症状改善情况,利用磁敏感成像技术(susceptibility-weighted imaging,SWI)侧支血管分级标准评估丁苯酞对缺血梗死区侧支循环的影响,并对结果加以分析。结果对照组与治疗组的症状与体征均有一定程度的改善,治疗组的改善程度明显高于对照纽,差异有统计学意义(P<0.05);治疗纽的神经功能缺损程度评分情况优于对照组,差异有统计学意义(P<0.05);对照组与治疗组SWI侧支血管显示分级均有提高,但治疗组患者提高例数显著多于对照组,差异有统计学意义(P<0.05);治疗过程中2组患者均未出现明显不良反应。结论丁苯酞治疗大面积脑梗死预后效果较好,可有效改善神经功能缺损,促进缺血梗死区侧枝循环重建。展开更多
文摘Phthalides represent an important class of bioactive heterocycle extensively found in pharmaceuticals and natural products,their syntheses have attracted extensively attention.A water-promoted and rhodium-catalyzed[3+2]tandem cyclization of aromatic acids and acrylates has been developed in air and neat water free of any additives,which provides an environmentally benign approach for constructing phthalide motifs.Compared with previous literatures,this methodology features quite simple reaction conditions,simple operation and additive-free.Mechanistic studies indicate that apart from the many other well-known oxidations of Rh(I)by external oxidant,hydrogen transfer with the acrylate being a hydrogen acceptor is involved to regenerate the active Rh species,which is different from documented metal-catalyzed phthalides syntheses.The application of this protocol is further demonstrated by the green synthesis of biologically active isoochracinic acid in one step.
文摘Transition-metal catalyzed cross-coupling is one of the basic strategies for the C-C bond formation.However,it is difficult to achieve satisfactory results when terminal alkynes with electron-withdrawing group such as propiolate esters are used.The reason behind this might be the easy polymerization of this type of alkynes in the presence of base.A tetrahydroxydiboron and copper sulfate co-promoted cross-coupling/cyclization of propiolate esters and o-iodobenzoic acid for the facile and efficient construction of phthalides is described.Preliminary mechanism study indicates that tetrahydroxydiboron can inhibit the polymerization of propiolate esters and increase the reaction rate.This method is characterized by high regio-and stereoselectivities,mild reaction conditions,short reaction time,broad substrate scope,and excellent functional group compatibility.
文摘An efficient and facile method for the synthesis of 3-indolyl-substituted phthalides by Friedel-Crafts alkylation of indoles with 3-hydroxyisobenzofuran-1(3H)-one has been developed. Using only 2 mol-% TsOH·H2O as the catalyst, various substituted indoles can react smoothly at room temperature to give the corresponding phthalides products in good to excellent yields (up to 96%).
文摘目的探讨丁苯酞对大面积脑梗死预后的影响。方法选取201 1年2月~2013年12月期间,在哈励逊国际和平医院神经内科住院的大面积脑梗死患者92例作为研究对象,采用对照研究。将患者随机分为对照组(n=46)和治疗组(n=46)。对照组给予依达拉奉注射液静脉滴注,治疗组在此基础上给予丁苯酞胶囊联合治疗。2组患者均持续给药,疗程为2周。利用神经功能缺损程度评分(national institute of health stroke scale,NIHSS)^([1])评定2组患者症状改善情况,利用磁敏感成像技术(susceptibility-weighted imaging,SWI)侧支血管分级标准评估丁苯酞对缺血梗死区侧支循环的影响,并对结果加以分析。结果对照组与治疗组的症状与体征均有一定程度的改善,治疗组的改善程度明显高于对照纽,差异有统计学意义(P<0.05);治疗纽的神经功能缺损程度评分情况优于对照组,差异有统计学意义(P<0.05);对照组与治疗组SWI侧支血管显示分级均有提高,但治疗组患者提高例数显著多于对照组,差异有统计学意义(P<0.05);治疗过程中2组患者均未出现明显不良反应。结论丁苯酞治疗大面积脑梗死预后效果较好,可有效改善神经功能缺损,促进缺血梗死区侧枝循环重建。
