Expeditious synthesis of dihydronaphthofurans utilising 1,2-dioxines and stabilised phosphorus ylides
作者:Thomas D. Haselgrove、Martyn Jevric、Dennis K. Taylor、Edward R.T. Tiekink
DOI:10.1016/s0040-4020(99)00919-9
日期:1999.12
A new practical synthesis of functionalised 1,2-dihydronaphtho[2,1-b]furans from substituted 2,4a-dihydronaphtho[2,1-c][1,2]dioxines and stabilised phosphorus ylides is described. Functionalised γ-hydroxy enones and their isomeric hemiacetals are key intermediates.
官能化的1,2-二氢萘并[2,1-的新型实用的合成b ]呋喃从取代的2,4-一个-dihydronaphtho [2,1- c ^ ] [1,2]二喔星和稳定的磷内鎓盐进行说明。功能化的γ-羟基烯酮及其异构半缩醛是关键中间体。
DDQ induced oxidative cyclisations of 1,2-dihydronaptho[2,1-b]furans
作者:Martyn Jevric、Dennis K. Taylor、Ben W. Greatrex、Edward R.T. Tiekink
DOI:10.1016/j.tet.2004.12.010
日期:2005.2
The DDQ mediated oxidative cyclisation reactions of a series of dihydronaptho[2,1-b]furans were examined. In the presence of an acid catalyst, the reaction yielded polycyclic ethers and lactones in good to excellent yields. (C) 2005 Elsevier Ltd. All rights reserved.
2-OXAZOLAMINES AND THEIR USE AS 5-HT2B RECEPTOR ANTAGONISTS
申请人:Pharmagene Laboratories Ltd
公开号:EP1474140A1
公开(公告)日:2004-11-10
[EN] 2-OXAZOLAMINES AND THEIR USE AS 5-HT2B RECEPTOR ANTAGONISTS<br/>[FR] 2-OXAZOLAMINES ET LEUR UTILISATION COMME ANTAGONISTES DU RECEPTEUR 5-HT2B
申请人:PHARMAGENE LAB LTD
公开号:WO2003068226A1
公开(公告)日:2003-08-21
The present invention relates to compounds of formula (I): wherein one of R1 and R4 is selected from the group consisting of H, and optionally substituted C1-6 alkyl, C3-7 cycloalkyl, C3-7 cycloalkyl-C1-4 alkyl, and phenyl-C1-4 alkyl; and the other of R1 and R4 is an optionally substituted C9-14 aryl group; R2 and R3 are either:(i) independently selected from H, R, R', SO2R, C(=O)R, (CH2)nNR5R6, where n is from 1 to 4 and R5 and R6 are independently selected from H and R, where R is optionally substituted C1-4 alkyl, and R' is optionally substituted phenyl-C1-4 alkyl, or (ii) together with the nitrogen atom to which they are attached, form an optionally substituted C5-7 heterocyclic group; and their use as pharmaceuticals, in particular for treating conditions alleviated by the antagonism of a 5-HT2B receptor.