The present invention relates to compounds of formula ##STR1## and the pharmaceutically acceptable salts thereof which are potent antagonists of PAF and are useful in the treatment of PAF-related disorders including asthma, shock, respiratory distress syndrome, acute inflammation, transplanted organ rejection, gastrointestinal ulceration, allergic skin diseases, delayed cellular immunity, parturition, fetal lung maturation, and cellular differentiation.
Ketone Synthesis under Neutral Conditions. Cu(I) Diphenylphosphinate-Mediated, Palladium-Catalyzed Coupling of Thiol Esters and Organostannanes
作者:Rüdiger Wittenberg、Jiri Srogl、Masahiro Egi、Lanny S. Liebeskind
DOI:10.1021/ol034962x
日期:2003.8.1
[reaction: see text] A versatile approach to ketone synthesis is described. The reaction relies on the palladium-catalyzed, copper diphenylphosphinate-mediated coupling of thiol esters with organostannanes under neutral reaction conditions. This reaction complements the previously described coupling of thiol esters with boronic acids that used dual thiophilic-borophilic activation methodology.
Fused heterotricyclic compounds, process for preparing the compounds and drugs containing the same
申请人:——
公开号:US20030078277A1
公开(公告)日:2003-04-24
The present invention provides a novel compound having an excellent corticotrophin-releasing-factor receptor antagonistic activity. That is, it provides a compound represented by the following formula, a pharmacologically acceptable salt thereof or hydrates thereof.
1
Wherein A, B and D are the same as or different from each other and each represents a group represented by the formula —(CR
1
R
2
)
m
— (wherein R
1
and R
2
are the same as or different from each other and each represents a C
1-6
alkyl group etc.), —NR
3
— (wherein R
3
represetns hydrogen etc.) etc.; E and G are the same as or different from each other and each represents a group represented by the formula —(CR
6
R
7
)
p
— (wherein R
6
and R
7
are the same as or different from each other and each represents hydrogen etc.; and p represents an integer of 0, 1 or 2); J represents a carbon atom or nitrogen atom, each substituted with C
1-6
alkyl group optionally substituted with a halogen atom, etc.; K and L are the same as or different from each other and each represents carbon atom or nitrogen atom; M means hydrogen, a halogen atom, an optionally substituted C
1-6
alkyl group etc.; and the partial structure
means a single or double bond.
Double insertion of alkynes into the C–Sn bond of an alkynyl-, alkenyl-, allyl- or arylstannane proceeded in the presence of a palladium–diimine complex to afford highlyconjugatedalkenylstannanes with exclusive syn selectivity. Perfect regioselectivities were observed in the dimerization–carbostannylation of ethyl propiolate with a palladium–1,2-bis[(2,6-diisopropylphenyl)imino]acenaphthene complex
SYNTHESIS AND REGIOSELECTIVE SUBSTITUTION OF 6-HALO-AND 6-ALKOXY NICOTINE DERIVATIVES
申请人:Comins Daniel L.
公开号:US20070232665A1
公开(公告)日:2007-10-04
The present invention provides active compounds for modulating nicotinic acetylcholine receptors and methods of making the same. The methods of preparing the active compounds utilize different intermediate compounds.