Sulfones as Synthetic Linchpins: Transition‐Metal‐Free sp
<sup>3</sup>
–sp
<sup>2</sup>
and sp
<sup>2</sup>
–sp
<sup>2</sup>
Cross‐Couplings Between Geminal Bis(sulfones) and Organolithium Compounds
作者:Barry M. Trost、Christopher A. Kalnmals
DOI:10.1002/chem.201800118
日期:2018.6.26
carbon of the bis(phenylsulfonyl)methyl unit to ultimately generate trisubstituted alkenes, comprising formal sp3–sp2 and sp2–sp2 cross‐couplings between organolithium reagents and bis(sulfones). This process occurs almost instantaneously at −78 °C in the absence of any transition metals. By developing this curious transformation, it has been demonstrated that bis(phenylsulfonyl)methane is a valuable
Substituted isoquinoline-1,3(2H,4H)-diones, 1-thioxo-1,4-dihydro-2H-isoquinoline-3-ones and 1,4-dihydro-3 (2H)-isoquinolones and methods of use thereof
申请人:Tsou Hwei-Ru
公开号:US20080085890A1
公开(公告)日:2008-04-10
This invention provides compounds of Formula (I), having the structure
where G
1
, G
2
, G
3
, G
4
, A
1
, A
2
, Y
1
, Y
2
, L
1
, Z, e and f are defined herein, or a pharmaceutically acceptable salt thereof, which are useful for treating or preventing cancer.
New synthetic methods were developed for the preparation of 2,3,6-trisubstituted 1-oxo-1,2-dihydroisoquinolines as CRTh2 antagonists. The isoquinolinone core could be constructed before the introduction of substitution groups or synthesized through a catalytic intramolecular cyclization reaction with desired substitution groups properly installed. These synthetic strategies have helped to accelerate
Synthesis of Isoindoles from Intramolecular Condensation of Benzyl Azides with α-Aryldiazoesters
作者:Jing Zhu、Rui Li、Yan Su、Peiming Gu
DOI:10.1021/acs.joc.8b03180
日期:2019.5.3
Rh-catalyzed intramolecular condensation of the benzyl azides with α-aryldiazoesters was explored. The reaction proceeded through the nucleophilic attack of the organic azide onto a rhodium carbenoid, while releasing nitrogen gas, affording the α-imino esters as the primary product. Tautomerization of the imino esters efficiently gave 13 desired isoindoles with good to excellent yields.
The present invention relates to isoquinolinone derivatives of formula (I):
wherein R
1
, R
2
, R
3
, R
4
, R
5
, R
6
and R
7
are as herein defined; processes for their preparation, pharmaceutical compositions containing them and their use in therapy.