标题化合物为P(3)轴向和P(3)赤道取代的顺式和反式构型9-苄基-3-氟-2,4-二氧杂-9-氮杂-3-磷酸钙素3-氧化物( = 9-苄基-3-氟-2,4-二氧杂-9-氮杂-3-磷酸双环[4.4.0]癸烷3-氧化物= 7-苄基-2-氟六氢-4 H -1,3,2-二氧杂磷基制备[4,5 - c ]吡啶2-氧化物)(ee> 99%)并充分表征(方案2和4)。绝对构型由其前体,对映体纯的1-苄基3-羟基哌啶4-羧酸乙酯和1-苄基3-羟基哌啶-4-甲醇分配而得。作为乙酰胆碱的结构固定和构象受限的磷类似物,标题化合物代表乙酰胆碱模拟物,是研究与乙酰胆碱酯酶的分子相互作用的合适探针。通过动力学方法确定,所有化合物都是该酶的中度不可逆抑制剂。
[EN] NOVEL 3-INDOL SUBSTITUTED DERIVATIVES, PHARMACEUTICAL COMPOSITIONS AND METHODS FOR USE<br/>[FR] NOUVEAUX DÉRIVÉS SUBSTITUÉS PAR UN 2-INDOLE, COMPOSITIONS PHARMACEUTIQUES ET LEURS PROCÉDÉS D'UTILISATION
申请人:PFIZER
公开号:WO2016147144A1
公开(公告)日:2016-09-22
A compound of Formula I is provided: or pharmaceutically acceptable enantiomers, salts or solvates thereof. The 5 invention further relates to the use of the compounds of Formula I as TDO2 inhibitors. The invention also relates to the use of the compounds of Formula I for the treatment and/or prevention of cancer, neurodegenerative disorders such as Parkinson's disease, Alzheimer's disease and Huntington's disease, chronic viral infections such as HCV and HIV, depression, and obesity. The invention also 10 relates to a process for manufacturing compounds of Formula I.
Convenient synthesis of anionic dinuclear ruthenium(II) complexes [NR2H2][{RuCl(diphosphine)}2(μ-Cl)3] [diphosphine=2,2′-bis(diphenylphosphino)-1,1′-binaphthyl, 2,2′-bis(di(p-tolyl)phosphino)-1,1′-binaphthyl, and 1,2-bis(diphenylphosphino)benzene]: crystal structure of [NEt2H2][{RuCl(1,2-bis(diphenylphosphino)benzene)}2(μ-Cl)3]
作者:Kazushi Mashima、Tomoko Nakamura、Yutaka Matsuo、Kazuhide Tani
DOI:10.1016/s0022-328x(00)00192-3
日期:2000.8
[NR2H2][RuCl(diphosphine)}2(μ-Cl)3]. A one-pot mixture of BINAP or its derivative, [RuCl2(η6-arene)]2, and NR2H2Cl produced salts of the anionicdinuclearcomplexes which can be applied as catalysts for the asymmetrichydrogenation of ketonic substrates such as acetol and methyl acetoacetate with high activity and high enantioselectivity. The anionic face-sharing bioctahedral structure of these complexes
[EN] PROCESS FOR THE PREPARATION OF RAMELTEON<br/>[FR] PROCÉDÉ DE PRÉPARATION DE RAMELTEON
申请人:RANBAXY LAB LTD
公开号:WO2011027323A1
公开(公告)日:2011-03-10
The present invention relates to a process for the preparation of ramelteon using 2- [(8S)-1, 6,7, 8-tetrahydro-2H-indeno[5,4-b]furan-8-yl]ethanamine of Formula I or a salt thereof as an intermediate.