The present description relates to fused polycyclic 2-pyridinone compounds and forms and pharmaceutical compositions thereof and methods of using such compounds, forms or compositions thereof for treating or ameliorating a wild-type or drug-resistant form of N. gonorrhoeae or N. meningitides. A compound of Formula (la), Formula (lb) or Formula (Ic), or a form thereof, wherein the dashed lines represent one or more double bonds optionally present where allowed by available valences.
Rhodium(I)-Catalyzed Cycloisomerization
of 1,3-Dienes with Alkenes in a Tether
作者:Yoshihiro Oonishi、Akira Saito、Miwako Mori、Yoshihiro Sato
DOI:10.1055/s-0028-1087973
日期:——
A rhodium(I)-catalyzedcycloisomerization of 1,3-dienes with alkenes in a tether proceeded smoothly, giving cyclopentene or cyclohexene derivatives in good yields. The existence of a hetero atom between the 1,3-diene moiety and the olefin in the tether affected the reaction course. In the case of the substrate having no hetero atom between the 1,3-diene moiety and olefin in the tether, cycloisomerization
[EN] NOVEL CYCLOSPORIN DERIVATIVES AND USES THEREOF<br/>[FR] NOUVEAUX DÉRIVÉS DE CYCLOSPORINE ET LEURS UTILISATIONS
申请人:S&T GLOBAL INC
公开号:WO2017200984A1
公开(公告)日:2017-11-23
A compound of the Formula (I) is disclosed: (I) or pharmaceutically acceptable salt thereof, wherein the symbols are as defined in the specification. Also described are a pharmaceutical composition comprising the same and a method for treating or preventing viral infections, inflammation, dry eye, central nervous disorders, cardiovascular diseases, cancer, obesity, diabetes, muscular dystrophy, lung, and liver, and kindey diseases, and hair loss using the same.
Synthesis of pentacyclic pyrrolo[3,4-a]carbazole-1,3(2H)-diones via an intermolecular Diels–Alder, intramolecular carbonyl-ene reaction strategy
作者:Matokah Abualnaja、Paul G. Waddell、William Clegg、Michael J. Hall
DOI:10.1016/j.tet.2016.08.008
日期:2016.9
intermolecular Diels–Alder (D–A) reaction between an N-protected 3-vinyl-1H-indole and N-methyl-maleimide, and a Lewis acid-catalysed intramolecular carbonyl-ene cyclisation reaction. Cyclopentyl- or cyclohexyl-containing scaffolds can be formed through variation in the length of the alkyl tether, whilst the observed stereospecificity of carbonyl-ene cyclisation supports a concerted mechanism.
五环吡咯并[3,4- a ]咔唑-1,3(2 H)-二酮是通过两个关键的合成步骤获得的,即N保护的3-乙烯基-1 H之间的分子间狄尔斯-阿尔德(D–A)反应-吲哚和N-甲基-马来酰亚胺,以及路易斯酸催化的分子内羰基-烯环化反应。含环戊基或环己基的支架可以通过改变烷基系链的长度来形成,而所观察到的羰基-烯环化的立体特异性则支持协同机制。
Diastereoselective synthesis of functionalised carbazoles via a sequential Diels–Alder/ene reaction strategy
作者:Joseph Cowell、Matokah Abualnaja、Stephanie Morton、Ruth Linder、Faye Buckingham、Paul G. Waddell、Michael R. Probert、Michael J. Hall
DOI:10.1039/c5ra00499c
日期:——
An operationally simple one-pot, three-component, diastereoselective synthesis of saturated carbazoles and related pyridazino[3,4-b]indoles, based on two sequential intermolecular pericyclic reactions, is described. The reaction sequence involves an intermolecular Diels–Alder (D–A) reaction of a 3-vinyl-1H-indole, containing an electron withdrawing N-protecting group, with a suitable dienophile. Due
描述了基于两个连续的分子间周环反应的操作简单的一锅,三组分,非对映选择性合成饱和咔唑和相关哒嗪并[3,4- b ]吲哚的方法。反应序列涉及3-乙烯基-1 H-吲哚的分子间Diels-Alder(D-A)反应,其中含有吸电子的N-保护基团和合适的亲二烯体。由于N保护基的吸电子特性,所得的D–A环加合物具有足够的稳定性,可在随后的原位非对映特异性分子间烯键反应下与添加的亲烯基团发生反应,从而生成相对立体控制最多为4的官能化咔唑立体中心。