Total synthesis of cannabisin F

A practical eight-step synthesis of lignanamide cannabisin F starting from vanillin is reported for the first time. This synthetic strategy applies the aldol reaction followed by the Wittig reaction to afford the key 8-O-4′-neolignan intermediate diacid. The diacid was condensed with N,O-protected tyramine giving, after deprotection, cannabisin F.     

硅花园法合成硅酸铝质子酸

A series of aluminasilicate Br?nsted acid catalysts were synthesized with the “silica garden” method, and characterized with XRD, XPS and NH₃-TPD technique. Acid center concentration was measured using ionic ex-change method. The catalytic activities for cumene cracking of the silica garden Br?nsted acid catalysts were ob-served and compared to that of zeolite HY and traditional acidic aluminasilicate catalysts. It was found that the 6-coordinate and 4-coordinate aluminum atoms were in silica garden Br?nsted acid catalysts. There were two kinds of acid centers and a little of crystal in silica garden Br?nsted acid catalysts. And it was also found that the crystal increased the acidities of the catalysts. The catalytic activity and strong acid center concentration of the silica garden Br?nsted acid catalysts were between that of zeolite HY and traditional acidic aluminasilicate catalysts.     

meso-去甲二氢愈创木酸和Machilin A的合成

报道了一条合成内消旋去甲二氢愈创木酸(meso-NDGA)和Machilin A的新路线. 此路线通过两次Stobbe缩合构建木脂素结构骨架, 经官能团转换, 合成了meso-NDGA和Machilin A. 该路线操作简便、实用性强.     

Facile Synthesis of Reduced Graphene Oxide-octahedral Mn3O4 Nanocomposites as a Platform for the Electrochemical Determination of Metronidazole and Sulfamonomethoxine

A facile synthesis strategy of reduced graphene oxide (RGO)-octahedral Mn₃O₄ (oct-Mn₃O₄) nanocomposites using in situ one-pot hydrothermal reaction was reported. The RGO-oct-Mn₃O₄ nanocomposites were drop-casted onto the surface of glassy carbon electrode (GCE) to obtain RGO-oct-Mn₃O₄/GCE. DPV results revealed that the performance of RGO-oct-Mn₃O₄/GCE towards metronidazole displayed a linear ranging from 0.1 to 9.5 μM with a detection limit of 0.037 μM. For sulfamonomethoxine, it exhibited a linear ranging from 1 to 95 μM with a detection limit of 0.27 μM. Moreover, the proposed sensor had good anti-interference capability, high stability, satisfactory reproducibility, and was successfully applied in real samples.     

Total Synthesis of (-)-Kaerophyllin,(-)-Hinokinin and (±)-Isohinokinin

Kaerophyllin (1) ,hinokinin (2 )andtheiranalogue isohinokinin (3)belongtothedibenzylbutyrolactone lig nans .Kaerophyllin (1)wasisolatedfromtherootofspot tedcowparsley (ChaerophyllummaculatumWilld .) 1andhinokinin (2 )wasisolatedfromtheheartwoodofLiboce drusformosanaFlorin .2 AccordingtoMacRaeandTow ers ,3afivememberedlactoneringandamethylenedioxylgroupwereimportantstructuralcharacteristicswhichcon tributetotheactivityoflignansasantitumoragents .More over ,anunsaturateddoublebondbetweenC3—…     

丁烷型木脂素及衍生物的合成和生物活性

报道了一条合成丁烷木脂素的新路线. 以芳香醛为起始原料, Stobbe缩合和烷基化反应为关键步骤, 构建了木脂素骨架, 再经拆分及还原, 可得到相应的苏式和赤式异构体. 经官能团转化得到5个丁烷木脂素和8个丁醚木脂素, 其中3个天然产物为首次合成. 对合成产物进行抗HIV病毒和和抗疱疹病毒活性研究, 部分化合物显示出较高的抗病毒活性, 而且骨架构型对活性影响较大.     

Threo-(±)-开环异落叶松脂醇二阿魏酸酯的全合成

报道了双木脂素threo-(±)-开环异落叶松脂醇二阿魏酸酯的全合成.以香草醛为原料,经过两步Sto-bbe反应构建木脂素骨架,然后再用LiAlH4还原、加氢后,产物经柱层析分离,得到2个异构体meso-和threo-(±)-开环落叶松脂素;根据其NMR,IR和HRMS等谱图确认发现,极性较小的产物threo-(±)-开环落叶松脂素为合成的关键中间体.threo-(±)-开环落叶松脂素与甲氧甲基(MOM)保护的阿魏酸缩合得到目标产物threo-(±)-开环异落叶松脂醇二阿魏酸酯.合成采用汇聚法,经11步,以约8%的总产率得到了目标产物.该合成方法具有原料价廉易得及操作简便的优点,并具有一定的实用价值.     

Threo-(±)-开环异落叶松脂醇二阿魏酸酯的全合成

报道了双木脂素threo-(±)-开环异落叶松脂醇二阿魏酸酯的全合成. 以香草醛为原料, 经过两步Stobbe反应构建木脂素骨架, 然后再用LiAlH₄还原、加氢后, 产物经柱层析分离, 得到2个异构体meso-和threo-(±)-开环落叶松脂素; 根据其NMR, IR和HRMS等谱图确认发现, 极性较小的产物threo-(±)-开环落叶松脂素为合成的关键中间体. threo-(±)-开环落叶松脂素与甲氧甲基(MOM)保护的阿魏酸缩合得到目标产物threo-(±)-开环异落叶松脂醇二阿魏酸酯. 合成采用汇聚法, 经11步, 以约8%的总产率得到了目标产物. 该合成方法具有原料价廉易得及操作简便的优点, 并具有一定的实用价值.     

(-)-(1R,2S)-肉豆蔻木脂素的不对称合成

报道了天然产物(-)-肉豆蔻木脂素的全合成. 以香草醛为起始原料, 经Wittig反应、LiAlH₄还原和Sharplass不对称双羟化等反应构建了苏式结构的中间体; 以焦性没食子酸为原料, 经Claisen重排反应制得另一种苯丙素片段; 2个中间体通过Mitsunobu反应, 缩合并使构型翻转, 得到赤式-(-)-肉豆蔻木脂素. 为赤式8-O-4′新木脂素的合成提供了一种新方法.     

天然产物(±)-Aiphanol的全合成研究

以醛1和5为起始原料,经几步反应后用Ag₂O偶联,得到含苯并二氧六环骨架的化合物7,化合物7经过选择性保护酚羟基,再用NaIO₄/OsO₄(cat.)氧化断裂双键,得到关键中间体9,化合物9和10经过Wittig-Horner反应,并用苯硫酚和AIBN实现了顺式双键向反式的转化,脱去保护基后完成了具有新颖结构的天然产物(±)-Aiphanol(12)的合成.