Study on the Synthesis of Metabolite CM2 of Clausenamide

Synthesis of the optically active metabolite of clausenamide CM2 (3, 5-dihydroxy- 5-(a-hydroxylbenzyl)-1-methyl-4-benzylpyrrolidin-2-one) from 3-O-acetyl- clausenamide was described.

Synthesis and biological evaluation of novel 2,4,5-triaryl-1 H-pyrazol-3(2H)-ones as inhibitors of ALK5

一系列 2,4,5-triaryl 在 vitro 作为 ALK5 禁止者代替了 1H-pyrazol-3 (2H )-ones, ，是 desigened，综合并且评估。大多数混合物在 1 μ m ol/L 展出了显著 ALK5 抑制活动并且没在 30 μ m ol/L 显示重要 cytotoxicities。

Synthesis and Biological Evaluation of Novel 1, 5-Diarylpyrazole-3- carboxamide Compounds as Inhibitors of ALK5

Ten new 1, 5-diarulpyrazole-3-carboxamide compounds were synthesized and their structures were identified by ^1H-NMR and FAB-MS. The primary biological tests showed that compound 4j exhibited some ALK5 inhibitory activity at concentration of 1μmol/L.

Asymmetric Synthesis of (-)-(4R, 5R)-4-[5-(Benzo[1, 3]dioxol-5-yl)-4- hydroxyl-1-(pyridin-2-yl)-4, 5-dihydro-1H-pyrazol-3-yl]benzamide

The asymmetric synthesis of （-）-（4R, 5R）-4-[5-（benzo[1, 3]dioxol-5-yl）-4-hydroxyl-1- （pyridin-2-yl）-4,5-dihydro-lH-pyrazol-3-yl]-benzamide with improved Juliá-Colonna asymmetric epoxidation procedure as key step was described.