CYCLOPENTA[C]PYRROLE-2-CARBOXYLATE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF
申请人:Abouabdellah Ahmed
公开号:US20120095040A1
公开(公告)日:2012-04-19
The invention relates to compounds of the general formula (I) where: R
2
is a hydrogen or fluorine atom or a hydroxyl, cyano, trifluoromethyl, C
1-6
-alkyl, C
1-6
-alkoxy, or NR
8
R
9
group; m, n, o and p independently are a number from 0 to 3; A is a covalent bond, an oxygen atom, a C
1-6
-alkylene group or a —O—C
1-6
-alkylene group in which the end that is an oxygen atom is bonded to the R
1
group while the end that is an alkylene group is bonded to the carbon of the bicyclic compound; R
1
is an optionally substituted aryl or heteroaryl group; R
3
is a hydrogen or fluorine atom or a C
1-6
-alkyl or trifluoromethyl group; R
4
is an optionally substituted 5-membered heterocyclic compound; wherein the compounds can be in the state of a base or an acid addition salt. The invention can be used in therapeutics.
Gold-catalyzed intermolecular [4+1] spiroannulation <i>via</i> site-selective aromatic C(sp<sup>2</sup>)–H functionalization and dearomatization of phenol derivatives
作者:Yongfeng Li、Zhiqiong Tang、Junliang Zhang、Lu Liu
DOI:10.1039/d0cc01118e
日期:——
A novel gold(i)-catalyzed chemo- and site-selective cascade C–H functionalization/dearomatization of naphthols or phenols with o-alkynylaryl-α-diazoesters has been developed.
Chiral catalyst, process for preparing the same and its use in the oxidate coupling of naphthols
申请人:Gong Liuzhu
公开号:US20050256345A1
公开(公告)日:2005-11-17
The compound of this invention is a useful catalyst for the oxidative coupling of naphthol. Its originality lies in that it is a novel vanadium complex of Schiff's base formed by a chiral amino acid and a formyl biphenol or its derivative. Its axis chirality is induced to form by the chiral amino acid. It has the general formula:
where R represents a benzyl, an isopropyl, an isobutyl or a tertiary butyl and the configuration of the amino acid is R or S. The compound can catalyze oxidative coupling of naphthol or its derivative to form binaphthol or its derivatives with a high optical purity.
Highly Enantioselective Oxidative Couplings of 2-Naphthols Catalyzed by Chiral Bimetallic Oxovanadium Complexes with Either Oxygen or Air as Oxidant
作者:Qi-Xiang Guo、Zhi-Jun Wu、Zhi-Bin Luo、Quan-Zhong Liu、Jian-Liang Ye、Shi-Wei Luo、Lin-Feng Cun、Liu-Zhu Gong
DOI:10.1021/ja074322f
日期:2007.11.1
L-isoleucine and H8-binaphthol is highlyefficient at catalyzing the air-oxidized coupling of 2-naphthols with excellent enantioselectivities of up to 97% ee. 51V NMR study shows that the oxovanadium complexes have two vanadium(V) species. Kinetic studies, the cross-coupling reaction, and HRMS spectral studies on the reaction have been carried out and illustrate that two vanadium(V) species are both involved
Herein, we report a highly efficientorganocatalyticasymmetric synthesis of axially chiral biaryl phosphonates with p-quinone phosphonates and 2-naphthols via CPA-catalyzed asymmetric arylations. A series of chiral biaryl monophosphonates were obtained in excellent yields and enantioselectivities (up to 99% yield and 95% ee). This reaction could be operated at a gram scale with a low catalyst loading