The present invention provides a most suitable prodrug of a cinnamide compound. The prodrug is represented by Formula (I)
wherein R
a
and R
b
each denote a C1-6 alkyl group or the like; X
a
denotes a methoxy group or a fluorine atom; Y denotes a phosphono group or the like; and A denotes a cyclic lactam derivative.
本发明提供了一种桂皮酰胺化合物的最适宜的前药。该前药由式(I)表示,其中R
a
和R
b
分别表示C1-6烷基或类似物;X
a
表示甲氧基或氟原子;Y表示磷酸酯基团或类似物;A表示环内酰胺衍生物。
Modulators of muscarinic receptors
申请人:Makings R. Lewis
公开号:US20080015179A1
公开(公告)日:2008-01-17
The present invention relates to modulators of muscarinic receptors. The present invention also provides compositions comprising such modulators, and methods therewith for treating muscarinic receptor mediated diseases.
Catalytic alkylation reactions of weakly acidic carbonyl and related pronucleophiles such as amides, esters, and sulfonamides with substituted alkenes have been reported. In the presence of a strong Brønsted base catalyst system, potassium hexamethyldisilazide and 18-crown-6 ether, the desired reactions proceeded in high yields at ambient temperature with a wide substrate scope. These are atom-economical
A diastereo- and enantioselective Michael addition of chiral amide enolates to α, β-unsaturated esters a stereoelective synthesis of (+)-dehydroiridodiol and (−)-isodehydroiridodiol
(+)-Dehydroiridodiol and (−)-isodehydroiridodiol were synthesized stereoselectively using the diastereo- and enantioselective Michael addition of chiral amide enolates to α, β-unsaturatedesters.
Progress toward the Total Synthesis of Callipeltin A (I): Asymmetric Synthesis of (3<i>S</i>,4<i>R</i>)-3,4-Dimethylglutamine
作者:Bo Liang、Patrick J. Carroll、Madeleine M. Joullié
DOI:10.1021/ol006679t
日期:2000.12.1
[reaction:see text] During the totalsynthesis of the novel cyclic depsipeptide callipeltin A (1), the unit (3S,4R)-3,4-dimethylglutamine, was successfully synthesized by asymmetric Michael addition and subsequent electrophilic azidation. The key feature of this approach is the generation of three adjacent stereogenic centers using the same camphorsultam chiral auxiliary.