The generation and reactivity of N-substituted, stabilised α,β:γ,δ-unsaturated azomethine ylides
摘要:
The generation of N-substituted, stabilised azomethine ylides in the presence of N-phenylmaleimide gave the bicyclo[3.3.0] octane-3-carboxylate cycloadducts. In the absence of a dipolarophile, these azomethine ylides gave novel piperazine-6-carboxylates. (C) 2002 Elsevier Science Ltd. All rights reserved.
Intramolecular Cyclization of 3,3-Diarylpropenylamides of Electron-Deficient Alkenes: Stereoselective Synthesis of Functionalized Hexahydrobenzo[<i>f</i>
]isoindoles
Reaction of electron‐deficient alkenes with 3,3‐diaryl‐2‐propen‐1‐amines under the amide formation conditions gave the tricyclic compounds in sequential processes involving intramolecular Diels–Alder reaction. The reaction gave cis‐ and trans‐fused tricyclic compounds selectively, depending on the substituents on the benzene ring, reaction temperature and solvent.
Significant Enhancement of the Stille Reaction with a New Combination of Reagents—Copper(I) Iodide with Cesium Fluoride
作者:Simon P. H. Mee、Victor Lee、Jack E. Baldwin
DOI:10.1002/chem.200401162
日期:2005.5.20
The combination of copper(I) iodide and cesiumfluoridesignificantlyenhances the Stillereaction. After extensive optimisation, a variety of electronically unfavourable and sterically hindered substrates were coupled in very high yields under mild conditions.
Disclosed are novel compounds of formula (I)
wherein A
1
, A
2
, Ar, R
5
, R
6
, R
8
, M, Q, Y, Z, k, m and n are as defined in the specification. These compounds are useful in the treatment and/or prevention of conditions mediated by nuclear receptors, in particular the Peroxisome Proliferator-Activated Receptors (PPAR). Such conditions include diabetes and obesity.
ee) was prepared by cyclopropanation of 3,3-diphenyl-2-propen-1-ol 1 with Et2Zn and CH2I2 in the presence of a catalytic amount of (S)-2-(methanesulfonyl)amino-1-(p-toluenesulfonyl)amino-3-phenylpropane 2, followed by esterification with 3,5-dinitorobenzoyl chloride, recrystallization, and hydrolysis.
由(+)-2,2-二苯基环丙基甲醇3a(98%ee)分两步合成(R)-(+)-噻吩啉(95%ee ),将其在DMSO中用IBX氧化,然后在乙二胺中用乙二胺处理。存在的我2和K 2 CO 3在吨BuOH中。化合物(R)-(+)- 3a(98%ee)通过在催化量存在下,将3,3-二苯基-2-丙烯-1-醇1与Et 2 Zn和CH 2 I 2环丙烷化制备的(小号)-2-(甲磺酰基)氨基-1-(p甲苯磺酰)氨基-3-苯基丙烷2,然后用3,5-二硝基苯甲酰氯进行酯化,重结晶和水解。
[EN] NEW COMPOUNDS, THEIR PREPARATION AND USE<br/>[FR] NOUVEAUX COMPOSES, PREPARATION ET UTILISATION DE CES DERNIERS
申请人:NOVO NORDISK AS
公开号:WO2000063153A1
公开(公告)日:2000-10-26
The present invention relates to compounds of general formula (I) The compounds are useful in the treatment and/or prevention of conditions mediated by nuclear receptors, in particular the Peroxisome Proliferator-Activated Receptors (PPAR).