[EN] INHIBITORS OF CYSTATHIONINE BETA SYNTHASE TO REDUCE THE NEUROTOXIC OVERPRODUCTION OF ENDOGENOUS HYDROGEN SULFIDE<br/>[FR] INHIBITEURS DE LA CYSTATHIONINE BÊTA SYNTHASE UTILISABLES EN VUE DE LA RÉDUCTION DE LA SURPRODUCTION NEUROTOXIQUE DE SULFURE D'HYDROGÈNE ENDOGÈNE
申请人:FOND JEROME LEJEUNE
公开号:WO2013068592A1
公开(公告)日:2013-05-16
The invention is directed to inhibitors of cystathionine beta synthase which, among other biochemical effects, allow reduction of the neurotoxic overproduction of endogenous hydrogen sulphide. These compounds and pharmaceutical compositions containing them are useful for the prevention and treatment of cognitive disorders such as cognitive disorders in Down syndrome. The invention also relates to methods for preventing or treating cognitive disorders including cognitive disorders in Down Syndrome.
Asymmetric Hydrogenation of <scp>Tetrapyridine‐Type <i>N</i>‐Heteroarenes</scp> Using <scp>Phosphine‐Free</scp> Ruthenium Diamine Catalysts<sup>†</sup>
作者:Chenghao Li、Shu‐Xin Zhang、Yu Feng、Yan‐Mei He、Qing‐Hua Fan
DOI:10.1002/cjoc.202300477
日期:2023.12.15
Chiral ruthenium-catalyzed enantioselective hydrogenation of tetrapyridine-type N-heteroarenes was firstly developed. The partial reduction of adjacent tetraheteroaromatic substrates proceeded smoothly in the presence of phosphine-freechiralcationic ruthenium diamine complexes, affording unprecedented high reactivity, enantioselecitivity and diastereoselectivity (up to 93% yield, >99% ee and 92 :
首次开发了手性钌催化四吡啶型N-杂芳烃的对映选择性氢化反应。在无膦手性阳离子钌二胺配合物存在下,相邻四杂芳族底物的部分还原顺利进行,提供了前所未有的高反应活性、对映选择性和非对映选择性(产率高达 93%、>99% ee 和 92:8 dr )。手性四齿吡啶胺产物作为手性配体的潜在应用已在铜催化吲哚和硝基烯烃之间的不对称弗里德尔-克来福特烷基化反应中得到证明。
Facile Access to Ring-Fused Aminals via Direct α-Amination of Secondary Amines with o-Aminobenzaldehydes: Synthesis of Vasicine, Deoxyvasicine, Deoxyvasicinone, Mackinazolinone, and Ruteacarpine
Secondary amines undergo redox-neutral reactions with aminobenzaldehydes under conventional and microwave heating to furnish polycyclic aminals via amine alpha-amination/N-alkylation. This unique alpha-functionalization reaction proceeds without the involvement of transition metals or other additives. The resulting aminal products are precursors for various quinazolinone alkaloids and their analogues.
MANIPULATION OF THE RETINOIC ACID SIGNALING PATHWAY