Design, Synthesis and Antifungal Activity of 6-Fluoro-3,3a,4,5-tetrahydro-2H-pyrazolo[4,3-c]-quinoline-2-carboxamide Derivatives

A series of 6-fluoro-3,3a,4,5-tetrahydro-2H-pyrazolo[4,3-c]quinoline-2-carboxamide derivatives was designed based on the bioisosterism and combination principle in drug design. The target compounds were synthesized from substituted aniline through Michael addition, cyclization, Mannich reaction and condensation with 4-substituted semicarbazides, and the structures were confirmed by mass spectrometry（MS） and 1H NMR. The antifungal assay was carried out in vitro by two-fold dilution. The result shows that all the compounds are of antifungal activities against the tested fungi at different levels.

Stereoselective Synthesis of 2-(4-Hydroxyphenyl)-3-hydroxymethyl-1,4-benzodioxane-6-aldehyde—The Key Intermediate of Sinaiticin

2-(4-Hydroxyphenyl)-3-hydroxymethyl-1,4-benzodioxane-6-aldehyde 8,the key intermediate of sinaiticin 10,was synthesized in 6 step from caffeic acid 4 and 4- hydroxybenzsaldehyde 1.the coupling reaction is the key step.

Biocatalytic Synthesis of Highly Enantiopure 1,4-Benzodioxane-2-carboxylic Acid and Amide

Catalyzed by Rhodococcus erythropolis AJ270, a nitrile hydratase and amidase containing microbial whole-cell catalyst, at 10 ℃ and with the use of methanol as a co-solvent, nitrile and amide biotransformations produce 2S-1,4-benzodioxane-2-carboxamide and 2R-1,4-benzodioxane-2-carboxylic acid in high yields with excellent enantioselectivity.

怀中1号鲜地黄化学成分研究

采用Toyopreal HW-40C、Sephadex LH-20、硅胶和半制备液相等多种色谱学技术从怀中1号鲜地黄中分离得到20个化合物。根据理化性质与波谱数据鉴定其结构,分别为3-methyl-2-(hydroxymethyl)-4H-pyrone-4-one(1)、3-氨基-2-吡啶乙醇(2)、(5’S)-2-oxo-N-phenylpyrrolidine-3-carboxamide (3)、焦谷氨酸甲酯(4)、吲唑(5)、尿苷(6)、腺苷(7)、rehmanalkaloid C (8)、1-(3-乙基苯基)-1,2-乙二醇(9)、(3-乙基苯基)-1,2-乙二醇(10)、2-羟甲基苯基-1-O-β-D-葡萄糖苷(11)、玉叶金花苷酸甲酯(12)、11-methylforsythide (13)、7-去氧栀子新苷(14)、1-O-α-L-鼠李糖苷(1→6)-β-D-吡喃葡萄糖苷(15)、6-deoxy-D-mannono-1,4-lactone (16)、富马酸单甲酯(17)、daphneresinol (18)、二氢槲皮素(19)、rhamnopyranosyl vaniloyl (20)。其中化合物1为新化合物,命名为3-methyl-2-(hydroxymethyl)-4H-pyrone-4-one,化合物2和3为新天然产物,化合物4、5、9~11、13、14以及16~19是从地黄属中首次分离得到的。