Reaction of 1,5-benzothiazepine with N-protected glycine gives new a-amino-β-lactamderivatives of 1.5-benzothiazepine. The configuration and conformation of the products wereconfirmed by x-ray diffraction. The resu...Reaction of 1,5-benzothiazepine with N-protected glycine gives new a-amino-β-lactamderivatives of 1.5-benzothiazepine. The configuration and conformation of the products wereconfirmed by x-ray diffraction. The result further reveals that the reaction of 1.5-benzothiazepineswith derivatives of carboxylic acid stereospecific.展开更多
A series of novel 1,5-benzothiazepine derivatives containing COOC2H5/COONa groups at the C（2）-position were synthesized and evaluated for their antifungal and antibacterial activities by both disc diffusion and mini...A series of novel 1,5-benzothiazepine derivatives containing COOC2H5/COONa groups at the C（2）-position were synthesized and evaluated for their antifungal and antibacterial activities by both disc diffusion and minimal inhibition concentration （MIC） methods. Most of the compounds have been shown to have moderate to good antibacterial activity against S. aureus, S. epidermidis and excellent antifungal activity against C. albicans.展开更多
Mass spectrometric behaviour of 2,2a,3,4-tetrahydro-4-methyl-2a-phenyl-2-(thiophen-2-yl)-1H-azeto[2,1-d][1,5]benzothiazepin-1-one-5-oxide and 2,3-dihydro-2,4-diphenyl-1,5-benzothiazepine-1-oxide/-1,1-dioxide have been...Mass spectrometric behaviour of 2,2a,3,4-tetrahydro-4-methyl-2a-phenyl-2-(thiophen-2-yl)-1H-azeto[2,1-d][1,5]benzothiazepin-1-one-5-oxide and 2,3-dihydro-2,4-diphenyl-1,5-benzothiazepine-1-oxide/-1,1-dioxide have been studied with the aid of mass-analyzed ion kinetic energy spectrometry and accurate mass measurements under electron impact ionization. The monooxide derivatives showed a tendency to eliminate an alkene or an oxygen atom. 1H-Azeto[2,1-d][1,5]benzothiazepin-1-one-5-oxide could also eliminate the thiophen-2-ylketene molecule via a reverse [2+2] cycloaddition. 2,3-Dihydro-2,4-diphenyl-1,5-benzothiazepine-1-oxide/-1,1-dioxide could eliminate SO_2 or SO, respectively. The structure of 2,2a,3,4-tetrahydro-4-methyl-2a-phenyl-2-(thiophen-2-yl)-1H-azeto[2,1-d][1,5]benzothiazepin-1-one-5-oxide was identified on the basis of its fragmentation. The identification was supported by the fragmentations of model compound, 2,3-dihydro-2,4-diphenyl-1,5-benzothiazepine-1-oxide/-1,1-dioxide.展开更多
The reaction of two series of 2,3-dihydro-1,5-henzothiazepines Ⅰ with dichloro- carbene,gave azirino[2,1-d][1,5]benzothiazepines Ⅷ,azirino[2,1-e][1,6]benzothiazocines Ⅸ, pyrrolo[2,1-b][1,3]benzothiazoles Ⅹ,substit...The reaction of two series of 2,3-dihydro-1,5-henzothiazepines Ⅰ with dichloro- carbene,gave azirino[2,1-d][1,5]benzothiazepines Ⅷ,azirino[2,1-e][1,6]benzothiazocines Ⅸ, pyrrolo[2,1-b][1,3]benzothiazoles Ⅹ,substituted-cyclopropanes Ⅺ and 2H-1,4-benzothiazin-2-ones Ⅻ.The structures of these products were confirmed by the analytical and spectral data.Compound Ⅷ and Ⅸ are two new ring systems.展开更多
基于耦合模式比较计划第6阶段(CMIP6)中的全球气候模式的模拟结果,采用考虑模式性能和独立性结合(Climate model Weighting by Independence and Performance,ClimWIP)的加权方案进行中国区域气候的多模式集合预估及不确定性研究。结果...基于耦合模式比较计划第6阶段(CMIP6)中的全球气候模式的模拟结果,采用考虑模式性能和独立性结合(Climate model Weighting by Independence and Performance,ClimWIP)的加权方案进行中国区域气候的多模式集合预估及不确定性研究。结果表明,ClimWIP方案在历史阶段的模拟优于等权重方案,降低了多模式模拟的气候态偏差。温度指数的未来预估不确定性较大的区域主要集中在中国北方和青藏高原,而降水指数主要集中在华北和西北地区。ClimWIP方案的预估不确定性与等权重方案相比有所降低。ClimWIP方案预估的温度指数的增温大值区主要集中在中国北方和青藏高原;降水指数在西北和青藏高原增加最为显著。全球额外0.5℃增暖时,中国区域平均的温度指数变化更强,平均高于全球0.2℃,最低温在东北部分地区的额外增温甚至是全球平均的3倍;总降水额外增加5.2%;强降水额外增加10.5%。全球增暖2℃下,中国大部分区域温度指数较当前气候态增加可能超过1.5℃(概率>50%),在中国北方和青藏高原的部分地区增温超过1.5℃的可能性更大(概率>90%);总降水,强降水和连续干日在西北和华北增加幅度有可能超过10%、25%和-5 d(概率>50%)。展开更多
目的分析1.5 T MRI对子宫内膜癌术前分期的诊断价值。方法回顾性选取2019年1月至2023年12月就诊于新疆生产建设兵团第二师库尔勒医院妇科且临床资料完整的42例子宫内膜癌患者作为研究对象,术前均接受1.5 T MRI检查且影像学资料完整。以...目的分析1.5 T MRI对子宫内膜癌术前分期的诊断价值。方法回顾性选取2019年1月至2023年12月就诊于新疆生产建设兵团第二师库尔勒医院妇科且临床资料完整的42例子宫内膜癌患者作为研究对象,术前均接受1.5 T MRI检查且影像学资料完整。以术后病理分期结果为“金标准”,检验术前1.5 T MRI对子宫内膜癌分期的一致性及诊断效能。结果42例患者术后病理诊断检出Ⅰ期27例(64.29%)、Ⅱ期6例(14.29%)、Ⅲ期8例(19.05%)、Ⅳ期1例(2.38%);术前1.5 T MRI检出Ⅰ期25例(59.52%)、Ⅱ期9例(21.43%)、Ⅲ期6例(14.29%)、Ⅳ期2例(4.76%),与术后病理诊断结果的吻合度较强(Kappa=0.829);术前1.5 T MRI鉴别诊断子宫内膜癌Ⅰ期、Ⅱ期、Ⅲ期、Ⅳ期的准确度(95.24%、97.62%、92.86%、97.62%)、敏感度(92.59%、100.00%、75.00%、100.00%)、特异度(100.00、97.22%、97.06%、97.22%)较高;术前1.5 T MRI鉴别诊断Ⅰa期、Ⅰb期的敏感度为100%,特异度为83.33%,准确度为96.30%,与术后病理诊断的吻合度较强(Kappa=0.886)。结论1.5 T MRI在子宫内膜癌术前分期诊断中具有较高的吻合度,且各期诊断的准确度、敏感度及特异度均较高,并且在Ⅰ期的浸润程度评估中同样具有较高价值,可为临床子宫内膜癌患者术前病情诊断及手术方案的制定提供客观依据,临床应用价值较高。展开更多
The reactions of 2,3-dihydro-1,5-benzothiazepines with ethoxyearbonylcarbene undergo complex rearrangements to produce rlng-opening and ring contraction products. Previously it was presumed that the different products...The reactions of 2,3-dihydro-1,5-benzothiazepines with ethoxyearbonylcarbene undergo complex rearrangements to produce rlng-opening and ring contraction products. Previously it was presumed that the different products were formed via different mechanisms depending on the kind of substituents at the 2-position of 1,5-benzothiazepines. However, on the basis of the further detailed investigation, it was found that all 1,5-benzothiazepines can undergo the same rearrangement to yield both ring-opening and ring contraction products.展开更多
1, 5-Benzothiazepines 1 react with phenylacetyl chloride to give the title compounds.The structures of these new compounds were confirmed by elemental analysis, ~1H NMR, ^(13)C NMRand MS spectroscopy, and their config...1, 5-Benzothiazepines 1 react with phenylacetyl chloride to give the title compounds.The structures of these new compounds were confirmed by elemental analysis, ~1H NMR, ^(13)C NMRand MS spectroscopy, and their configuration (the mutual positions of the substituents relative to theβ-lactam ring) and conformation of the compounds were determined by X-ray crystal analysis.展开更多
The title compound -(N-protected amino)--lactam (C36H33N2O5ClS), derivative of 1,5-benzothiazepine, was prepared by the reaction of 1,5-benzothiazepine 1 with (4R)- phenyloxazolidylacetyl chloride and characteized by ...The title compound -(N-protected amino)--lactam (C36H33N2O5ClS), derivative of 1,5-benzothiazepine, was prepared by the reaction of 1,5-benzothiazepine 1 with (4R)- phenyloxazolidylacetyl chloride and characteized by X-ray diffraction analysis. The title compound crystallizes in orthorhombic system, space group P212121 with a=12.293(2), b=26.026(5), c=10.146(2)? V=3246.1?, Z=4, Dc=1.312g/cm3, Mr=641.15, F(000)=1344, μ= 0.228 mm1. The final R=0.0597 and wR=0.1165 for 3226 observed reflections with I ≥ 2?I). The crystal structure shows that the 4-phenyloxazolidyl and phenyl attached to C(8) and C(9) are in cis positions, and no trans product was discovered. So the cyclization to -lactam is stereospecific.展开更多
文摘Reaction of 1,5-benzothiazepine with N-protected glycine gives new a-amino-β-lactamderivatives of 1.5-benzothiazepine. The configuration and conformation of the products wereconfirmed by x-ray diffraction. The result further reveals that the reaction of 1.5-benzothiazepineswith derivatives of carboxylic acid stereospecific.
基金support from National Natural Science Foundation of China(No.20772021)the Natural Science Foundation of Hebei Province,China(No.2007000239)
文摘A series of novel 1,5-benzothiazepine derivatives containing COOC2H5/COONa groups at the C（2）-position were synthesized and evaluated for their antifungal and antibacterial activities by both disc diffusion and minimal inhibition concentration （MIC） methods. Most of the compounds have been shown to have moderate to good antibacterial activity against S. aureus, S. epidermidis and excellent antifungal activity against C. albicans.
文摘Mass spectrometric behaviour of 2,2a,3,4-tetrahydro-4-methyl-2a-phenyl-2-(thiophen-2-yl)-1H-azeto[2,1-d][1,5]benzothiazepin-1-one-5-oxide and 2,3-dihydro-2,4-diphenyl-1,5-benzothiazepine-1-oxide/-1,1-dioxide have been studied with the aid of mass-analyzed ion kinetic energy spectrometry and accurate mass measurements under electron impact ionization. The monooxide derivatives showed a tendency to eliminate an alkene or an oxygen atom. 1H-Azeto[2,1-d][1,5]benzothiazepin-1-one-5-oxide could also eliminate the thiophen-2-ylketene molecule via a reverse [2+2] cycloaddition. 2,3-Dihydro-2,4-diphenyl-1,5-benzothiazepine-1-oxide/-1,1-dioxide could eliminate SO_2 or SO, respectively. The structure of 2,2a,3,4-tetrahydro-4-methyl-2a-phenyl-2-(thiophen-2-yl)-1H-azeto[2,1-d][1,5]benzothiazepin-1-one-5-oxide was identified on the basis of its fragmentation. The identification was supported by the fragmentations of model compound, 2,3-dihydro-2,4-diphenyl-1,5-benzothiazepine-1-oxide/-1,1-dioxide.
文摘The reaction of two series of 2,3-dihydro-1,5-henzothiazepines Ⅰ with dichloro- carbene,gave azirino[2,1-d][1,5]benzothiazepines Ⅷ,azirino[2,1-e][1,6]benzothiazocines Ⅸ, pyrrolo[2,1-b][1,3]benzothiazoles Ⅹ,substituted-cyclopropanes Ⅺ and 2H-1,4-benzothiazin-2-ones Ⅻ.The structures of these products were confirmed by the analytical and spectral data.Compound Ⅷ and Ⅸ are two new ring systems.
文摘基于耦合模式比较计划第6阶段(CMIP6)中的全球气候模式的模拟结果,采用考虑模式性能和独立性结合(Climate model Weighting by Independence and Performance,ClimWIP)的加权方案进行中国区域气候的多模式集合预估及不确定性研究。结果表明,ClimWIP方案在历史阶段的模拟优于等权重方案,降低了多模式模拟的气候态偏差。温度指数的未来预估不确定性较大的区域主要集中在中国北方和青藏高原,而降水指数主要集中在华北和西北地区。ClimWIP方案的预估不确定性与等权重方案相比有所降低。ClimWIP方案预估的温度指数的增温大值区主要集中在中国北方和青藏高原;降水指数在西北和青藏高原增加最为显著。全球额外0.5℃增暖时,中国区域平均的温度指数变化更强,平均高于全球0.2℃,最低温在东北部分地区的额外增温甚至是全球平均的3倍;总降水额外增加5.2%;强降水额外增加10.5%。全球增暖2℃下,中国大部分区域温度指数较当前气候态增加可能超过1.5℃(概率>50%),在中国北方和青藏高原的部分地区增温超过1.5℃的可能性更大(概率>90%);总降水,强降水和连续干日在西北和华北增加幅度有可能超过10%、25%和-5 d(概率>50%)。
文摘目的分析1.5 T MRI对子宫内膜癌术前分期的诊断价值。方法回顾性选取2019年1月至2023年12月就诊于新疆生产建设兵团第二师库尔勒医院妇科且临床资料完整的42例子宫内膜癌患者作为研究对象,术前均接受1.5 T MRI检查且影像学资料完整。以术后病理分期结果为“金标准”,检验术前1.5 T MRI对子宫内膜癌分期的一致性及诊断效能。结果42例患者术后病理诊断检出Ⅰ期27例(64.29%)、Ⅱ期6例(14.29%)、Ⅲ期8例(19.05%)、Ⅳ期1例(2.38%);术前1.5 T MRI检出Ⅰ期25例(59.52%)、Ⅱ期9例(21.43%)、Ⅲ期6例(14.29%)、Ⅳ期2例(4.76%),与术后病理诊断结果的吻合度较强(Kappa=0.829);术前1.5 T MRI鉴别诊断子宫内膜癌Ⅰ期、Ⅱ期、Ⅲ期、Ⅳ期的准确度(95.24%、97.62%、92.86%、97.62%)、敏感度(92.59%、100.00%、75.00%、100.00%)、特异度(100.00、97.22%、97.06%、97.22%)较高;术前1.5 T MRI鉴别诊断Ⅰa期、Ⅰb期的敏感度为100%,特异度为83.33%,准确度为96.30%,与术后病理诊断的吻合度较强(Kappa=0.886)。结论1.5 T MRI在子宫内膜癌术前分期诊断中具有较高的吻合度,且各期诊断的准确度、敏感度及特异度均较高,并且在Ⅰ期的浸润程度评估中同样具有较高价值,可为临床子宫内膜癌患者术前病情诊断及手术方案的制定提供客观依据,临床应用价值较高。
文摘The reactions of 2,3-dihydro-1,5-benzothiazepines with ethoxyearbonylcarbene undergo complex rearrangements to produce rlng-opening and ring contraction products. Previously it was presumed that the different products were formed via different mechanisms depending on the kind of substituents at the 2-position of 1,5-benzothiazepines. However, on the basis of the further detailed investigation, it was found that all 1,5-benzothiazepines can undergo the same rearrangement to yield both ring-opening and ring contraction products.
文摘1, 5-Benzothiazepines 1 react with phenylacetyl chloride to give the title compounds.The structures of these new compounds were confirmed by elemental analysis, ~1H NMR, ^(13)C NMRand MS spectroscopy, and their configuration (the mutual positions of the substituents relative to theβ-lactam ring) and conformation of the compounds were determined by X-ray crystal analysis.
基金Supported by the Natural Foundation of Hebei Province
文摘The title compound -(N-protected amino)--lactam (C36H33N2O5ClS), derivative of 1,5-benzothiazepine, was prepared by the reaction of 1,5-benzothiazepine 1 with (4R)- phenyloxazolidylacetyl chloride and characteized by X-ray diffraction analysis. The title compound crystallizes in orthorhombic system, space group P212121 with a=12.293(2), b=26.026(5), c=10.146(2)? V=3246.1?, Z=4, Dc=1.312g/cm3, Mr=641.15, F(000)=1344, μ= 0.228 mm1. The final R=0.0597 and wR=0.1165 for 3226 observed reflections with I ≥ 2?I). The crystal structure shows that the 4-phenyloxazolidyl and phenyl attached to C(8) and C(9) are in cis positions, and no trans product was discovered. So the cyclization to -lactam is stereospecific.
