Stereochemistry and ring opening of a carbocyclic analogue of a 1-oxapenam
作者:Demetrios Agathocleous、Graham Cox、Michael I Page
DOI:10.1016/s0040-4039(00)84333-6
日期:1986.1
The cycloaddition of succinimido ketene to 2,3-dihydrofuran yields P--succinimido bicyclo [3.2.0] 2-oxoheptan-6-one. This unusual stereochemistry is confirmed by 1H NMR and X-ray crystallography. The cyclobutanone product undergoes ringopening in concentrated hydrochloric acid to give 1-succinimido-5-chloro-2-pentanone.
Synthesis of 4,5-Dihydro-1H-[1,2]dithiolo[3,4-c]quinoline-1-thione Derivatives and Their Application as Protein Kinase Inhibitors
作者:Svetlana M. Medvedeva、Khidmet S. Shikhaliev
DOI:10.3390/molecules27134033
日期:——
This study represents the design and synthesis of a new set of hybrid and chimeric derivatives of 4,5-dihydro-4,4-dimethyl-1H-[1,2]dithiolo[3,4-c]quinoline-1-thiones, the structure of which the tricyclic fragment linearly bound or/and condensed with another heterocyclic fragment. Using the PASS Online software, among the previously synthesized and new derivatives of 1,2-dithiolo[3,4-c]quinoline-1-thione
这项研究代表了一组新的 4,5-二氢-4,4-二甲基-1 H -[1,2]二硫醇[3,4- c ]喹啉-1-硫酮的杂化和嵌合衍生物的设计和合成,其中三环片段与另一个杂环片段线性结合或/和缩合的结构。使用 PASS Online 软件,在 1,2-二硫并[3,4- c ]喹啉-1-硫酮的先前合成和新衍生物中,我们鉴定了 12 种具有多效活性的物质,包括化学保护和抗肿瘤活性。所有合成的衍生物都经过筛选,以评估其对多种激酶的抑制作用。还通过ELISA检查了在细胞中表现出显着抑制百分比(>85%)的化合物对人激酶的抑制效率,使用索拉非尼作为参考标准来估计其IC 50值。结果表明,化合物2a 、 2b 、 2c和2q对JAK3具有显着的抑制作用(IC 50分别为0.36 μM、0.38 μM、0.41 μM和0.46 μM)。此外,化合物2a和2b对NPM1-ALK表现出优异的活性(IC 50分别为0
3β-(3,4-Disubstituted succinimido)azetidinones are provided via stereoselective cycloaddition of imines with chiral auxiliary 3,4-disubstituted succinimidoacetyl chlorides. The chiral auxiliary e.g., 3S,4S-dibenzoyloxy-and 3S,4S-diacetoxysuccinimidoacetyl chloride, is obtained from tartaric acid via anhydride and imide formation with retention of chirality. The chiral azetidinones obtained are useful intermediates to β-lactam antibacterial compounds.
The present invention aims to provide a novel compound effective as an antitumor active agent or vaccine adjuvant and an intermediate useful for the synthesis of the compound, as well as production methods thereof, and a medicament containing the novel compound.
A carbamate glycolipid represented by the formula (I)
wherein each symbol is as defined in the DESCRIPTION, and dendritic cell pulsed with the glycolipid.