Formal Total Synthesis of Kendomycin by Way of Alkyne Metathesis/Gold Catalysis
作者:Laura Hoffmeister、Peter Persich、Alois Fürstner
DOI:10.1002/chem.201304580
日期:2014.4.7
In an attempt to study the ability of the latest generation of alkyne metathesis catalysts to process sterically hindered substrates, two different routes to the bacterial metabolite kendomycin (1) were explored. Whereas the cyclization of the overcrowded arylalkyne 39 and related substrates turned out to be impractical or even impossible, ring closure of the slightly relaxed diyne 45 was achieved
Highlysolubleannelated bi- and terpyridines were prepared in 46–60% yields by a two-step procedure which combines the Michael addition of an enolizable cyclic ketone with an α,β-unsaturated ketone and the cyclization of the resulting 1,5-diketone in the presence of ammonium acetate.
The present invention relates to antiandrogenic compounds which may be administered for the treatment of androgen excess in the skin and by way of consequence, the treatment of acne, baldness or hirsuitism in subject or patient. These compounds have the general chemical structure I, II, III or IV:
or
Unexpected Cross-Coupling Reaction between <i>o</i>-Chloroaryl Ketones and Organomanganese Reagents
作者:Gérard Cahiez、Denis Luart、Fabien Lecomte
DOI:10.1021/ol048842g
日期:2004.11.1
Alkyl- and arylmanganese reagents react with o-chloro or o-bromoaryl ketones to give the substituted ketones in high yields. The cross-coupling reaction is performed under mild conditions (-60 to +40 degreesC, 30 min to 4 h) and takes place with excellent chemoselectivity.
LOCALLY ACTIVE "SOFT" ANTIANDROGENS
申请人:Hochberg Richard
公开号:US20100184735A1
公开(公告)日:2010-07-22
The present invention relates to antiandrogenic compounds which may be administered for the treatment of androgen excess in the skin and by way of consequence, the treatment of acne, baldness or hirsuitism in subject or patient. These compounds have the general chemical structure (I, II, III or IV):