有效地实现了布朗斯台德酸介导的内烯烃α-氧代乙烯酮二硫缩醛与吡咯的环化反应,得到环戊[ b ]吡咯。一对具有酸强度的布朗斯台德酸,即三氟乙酸和对甲苯磺酸水合物,被用于促进环化反应。生成的产物很容易被间氯过氧苯甲酸氧化成砜。随后用1,8-二氮杂双环[5.4.0]十一碳-7-烯处理得到脱硫的烯烃中间体脱硫的末端烯烃或[2 + 2]环加成产物。本协议提供了在温和条件下易于访问结构多样的环戊[ b ]吡咯衍生物的方法。
[EN] IMIDAZOLE COMPOUNDS AS MODULATORS OF FSHR AND USES THEREOF<br/>[FR] COMPOSÉS IMIDAZOLE SERVANT DE MODULATEURS DES RÉCEPTEURS DE LA FSHR ET LEURS UTILISATIONS
申请人:MERCK PATENT GMBH
公开号:WO2014209978A1
公开(公告)日:2014-12-31
The present invention relates to imidazole compounds, and pharmaceutically acceptable compositions thereof, useful as positive allosteric modulators of follicle stimulating hormone receptor (FSHR).
AMINOINDANE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM, AND THEIR USE IN THERAPY
申请人:POHLKI Frauke
公开号:US20120040948A1
公开(公告)日:2012-02-16
The present invention relates to aminoindane derivatives of the formula (I)
or a physiologically tolerated salt thereof.
The invention relates to pharmaceutical compositions comprising such aminoindane derivatives, and the use of such aminoindane derivatives for therapeutic purposes. The aminoindane derivatives are GlyT1 inhibitors.
1,8-naphthyridinone compounds as modulators of an adenosine receptor are provided. The compounds may find use as therapeutic agents for the treatment of diseases mediated through a G-protein-coupled receptor signaling pathway and may find particular use in oncology.
BF3·OEt2-mediated alkenylation of pyrroles with α-oxo ketene dithioacetals
作者:Xiaoge Yang、Kaikai Wu、Zhengkun Yu
DOI:10.1016/j.tetlet.2015.05.102
日期:2015.7
BF3·OEt2-mediated alkenylation of pyrroles with α-oxo ketene dithioacetals was efficiently realized, affording mono- and disubstituted ketene pyrrolyl acetals. In the cases of using N-unprotected pyrrole, the reactions gave ketene bipyrrolyl acetals as well as N,O-chelated BF2 complexes. Diverse C–S transformations were achieved for the monosubstituted products, yielding N-heterocycles or multisubstituted
Symmetrical diazo compounds containing 2-pyridinium groups and a cationic or non-cationic linker, compositions comprising them, method of coloring, and device
申请人:David Herve
公开号:US20060156488A1
公开(公告)日:2006-07-20
The present disclosure relates to symmetrical cationic diazo compounds of formula (I), the resonance forms, and also the acid addition salts and/or the solvates thereof:
The present disclosure further relates to dyeing compositions comprising such compounds as a direct dye in a medium appropriate for the dyeing of keratin fibers, and also to a method of coloring keratin fibers that employs this composition, and a multi-compartment kit containing such compositions.