Rhodium-Catalyzed Stereoselective Intramolecular [5 + 2] Cycloaddition of 3-Acyloxy 1,4-Enyne and Alkene
作者:Xing-zhong Shu、Casi M. Schienebeck、Xiaoxun Li、Xin Zhou、Wangze Song、Lianqing Chen、Ilia A. Guzei、Weiping Tang
DOI:10.1021/acs.orglett.5b02665
日期:2015.10.16
The first rhodium-catalyzedintramolecular [5 + 2] cycloaddition of 3-acyloxy 1,4-enyne and alkene was developed. The cycloaddition is highly diastereoselective in most cases. Various cis-fused bicyclo[5.3.0]decadienes were prepared stereoselectively. The chirality in the propargylic ester starting materials could be transferred to the bicyclic products with high efficiency. Electron-deficient phosphine
Pyrazolidinone compounds as ligands of the prostaglandin ep2 and/or ep4 receptors
申请人:——
公开号:US20040254233A1
公开(公告)日:2004-12-16
The invention provides substituted pyrazolidinone compounds, and methods of treatment and pharmaceutical compositions that utilize or comprise one or more such compounds. Compounds of the invention are useful for a variety of therapies, including treating or preventing preterm labor, dysmenorrhea, asthma, hypertension, infertility or fertility disorder, undesired blood clotting, preeclampsia or eclampsia, an eosinophil disorder, sexual dysfunction, osteporosis and other destructive bone disease or disorder, and other diseases and disorders associated with the prostaglandin EP2 and/or EP4 receptors.
A hydroxyfattysulfonic acid analog represented by Formula (I): wherein X is an ethylene group, a vinylene group or an ethynylene group; Y is an ethylene group, a vinylene group, an ethynylene group, OCH
2
or S(O)pCH
2
wherein p is 0, 1 or 2; m is an integer of 1 to 5 inclusive; n is an integer of 0 to 4 inclusive; R
1
is a C
1-8
alkyl group, a C
3-8
cycloalkyl group, a C
1-4
alkyl group substituted with a C
3-8
cycloalkyl group, a C
1-4
alkyl group substituted with an aryl group or a C
1-4
alkyl group substituted with an aryloxy group; R
2
is a hydrogen atom or a methyl group; R
1
and R
2
together with the carbon atom to which they are attached may form a C
3-8
cycloalkyl group; R
3
is a hydrogen atom or a C
2-8
acyl group; R
4
is OR
5
or NHR
6
, wherein R
5
is a hydrogen atom, a C
1-4
alkyl group, an alkali metal, an alkaline earth metal or an ammonium group and R
6
is a hydrogen atom or a C
1-4
alkyl group; or a pharmaceutically acceptable salt or a hydrate thereof. The compounds of the present invention are useful as an elastase release inhibitor.
PYRAZALIDINONE COMPOUNDS AS LIGANDS OF THE PROSTAGLANDIN EP2 AND/OR EP4 RECEPTORS
申请人:ARALDI Gian Luca
公开号:US20080234346A1
公开(公告)日:2008-09-25
The invention provides substituted pyrazolidinone compounds, and methods of treatment and pharmaceutical compositions that utilize or comprise one or more such compounds. Compounds of the invention are useful for a variety of therapies, including treating or preventing preterm labor, dysmenorrhea, asthma, hypertension, infertility or fertility disorder, undesired blood clotting, preeclampsia or eclampsia, an eosinophil disorder, sexual dysfunction, osteporosis and other destructive bone disease or disorder, and other diseases and disorders associated with the prostaglandin EP2 and/or EP4 receptors.