A new route to the synthesis of thieno[2,3-d]pyrimidin-4(3H)-one derivatives catalyzed by 12-tungstophosphoric acid (H_3PW_(12)O_(40))

Heteropoly acid H3PW12040 （PW） has been used as an effective catalyst for the synthesis of thieno[2,3-d]pyrimidin-4（3H）-one derivatives. The present methodology offers several advantages, such as high yields, short reaction times, mild reaction condition and a recyclable catalyst with a very easy work up.

H_3PMo_(12)O_(40) catalyzed three-component one-pot synthesis of 4,6-diarylpyrimidin-2(1H)-ones under solvent-free conditions

4,6-Diarylpyrimidin-2(1H)-one derivatives have been synthesized from three-component one-pot condensation of acetophe-none derivatives,aldehydes and urea in the presence of trimethylsilyl chloride and a catalytic amount of HPMoOunder solvent-free conditions.

Vitamin B12: An efficient type catalyst for the one-pot synthesis of 3,4,5-trisubstituted furan-2(5H)-ones and N-aryl-3-aminodihydropyrrol-2-one-4-carboxylates

Vitamin B12 was applied as catalyst for the one-pot three-component synthesis of 3,4,5-trisubstituted furan-2（5H）-ones from the condensation between aldehydes, amines and dialkylacetylendicarboxylates at ambient temperature in Et OH. In addition, N-aryl-3-aminodihydropyrrol-2-one-4-carboxylates were synthesised using mentioned catalyst at ambient temperature in Et OH from condensation between formaldehyde, amines, and dialkylacetylenedicarboxylates. This methodology has number of advantages such as： use of green and nonhazardous catalyst, clean work up, short reaction times,high yields and no need to column chromatography.

京大戟化学成分的研究

目的研究京大戟的化学成分。方法利用硅胶柱色谱、制备薄层等手段进行分离纯化,通过波谱数据分析和理化性质鉴定化合物结构。结果从京大戟中分离并鉴定了10个化合物,分别为二十四烷醇(1)、正十八烷醇(2)、十四烷酸(3)、大戟醇(4)、阿魏酸二十八酯(5)、β-谷甾醇(6)、(3β,12α,13α)-3,12-dihydroxypimara-7,15-dien-2-one(7)、pekinenal(8)、neomotiol(9)、3,3'-二甲氧基鞣花酸(10)。化合物7和8对人正常肝细胞LO2和人胃上皮GES-1细胞增殖具有抑制作用,化合物7对两种细胞的IC50为51.196μg/mL和21.223μg/mL;化合物8对两种细胞的IC50分别为15.722μg/mL和13.294μg/mL。结论化合物1、3、7、9为首次从该植物中发现。

Synthesis,Urease Inhibition and Molecular Modelling Studies of Novel Derivatives of the Naturally Occurring b-Amyrenone

Urease enzyme(UE)has been reported to be a potent virulence factor for Helicobacter pylori(HP)bacteria indicated to be responsible for various gastrointestinal diseases.Therefore,the spread of HP,currently regarded by the World Health Organization as a class 1 carcinogen,could be better controlled by targeting UE.It is in this line that we have synthesized three new derivatives(2–4)of the naturally occurring olean-12-en-3-one(1),which was previously isolated from the figs of Ficus vallis-choudae Delile(Moraceae).Among the synthesized compounds,3 and 4 contain an indole moiety.Their structures were unambiguously assigned by spectroscopic and spectrometric techniques(1D-NMR,2D-NMR and MS).The starting material and the synthesized compounds were screened for UE inhibition activity,and showed significant activities with IC50 values ranging from 14.5 to 24.6 lM,with compound(1)being the most potent as compared to the positive control thiourea(IC50=21.6 lM).Amongst the synthetic derivatives,compound 4 was the most potent(IC50-=17.9 lM),while the others showed activities close to that of the control.In addition,molecular docking study of target compounds 2–4 was performed in an attempt to explore their binding mode for the design of more potent UE inhibitors.

雷山石杉的化学成分研究

目的研究雷山石杉的化学成分。方法使用制备薄层、硅胶柱色谱、SephadexLH-20及半制备高效液相色谱法等手段进行分离、纯化，结合文献资料、理化性质、1H—NMR及13C-NMR数据进行结构鉴定。结果分离得到10个化合物，分别鉴定为（15R）-12，16-epoxy-11，14-dihydroxy-8，11，13-abietatrien-7-one（Ⅰ），21-epi—serratenediol-3，21-acetate（Ⅱ），setTatene—diol-3-acetate（Ⅲ），21-epi—serratenediol-3-acetate（Ⅳ），21a—hydroxy—serrat-14-en-3β-ol（Ⅴ），21β-hydroxy—serrat-14-en-3β-ol（Ⅵ），石杉碱甲（huperzineA，Ⅶ），蔗糖（Ⅷ），β-谷甾醇（Ⅸ），胡萝卜串（Ⅹ）。结论化合物Ⅰ～Ⅹ均首次从该植物中分离到。