SUBSTITUTED CYCLOPENTANES HAVING PROSTAGLANDIN ACTIVITY
申请人:Donde Yariv
公开号:US20090124676A1
公开(公告)日:2009-05-14
Disclosed herein are compounds having a formula:
Therapeutic methods, medicaments, and compositions related thereto are also disclosed.
本文揭示了具有以下化学式的化合物:还公开了与之相关的治疗方法、药物和组合物。
Biaromatic amido compounds and pharmaceutical/cosmetic compositions
申请人:Centre International de Recherches Dermatologiques Galderma
公开号:US05935585A1
公开(公告)日:1999-08-10
Novel pharmaceutically/cosmetically-active biaromatic amido compounds have the structural formula (I): ##STR1## in which Ar is a radical selected from among those of the following formulae (a)-(e): ##STR2## and are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders.
Novel asymmetric syntheses of (−)-malyngolide and (+)-epi-malyngolide
作者:Dieter Enders、Monika Knopp
DOI:10.1016/0040-4020(96)00236-0
日期:1996.4
diastereo- and enantioselective synthesis of (−)-malyngolide [(S, R)-1], an antibiotic against Mycobacterium smegmatis and Streptococcus pyogenes, using the asymmetric Carroll rearrangement as key step is described. Furthermore, the diastereo- and enantioselective synthesis by double α, α′-alkylation using SAMP/RAMPhydrazonemethodology affords the diastereomer (+)- epi-malyngolide [(S, S)-1].
Synthèse de composés cyclopentaniques chiraux, di, tri et tétrasubstitués. Application à la synthèse de dérivés Oxa-13-prostanoïques
作者:Jean-Claude Barrière、Jeanine Cléophax、Stephan D. Géro、Marc Vuilhorgne
DOI:10.1002/hlca.19830660508
日期:1983.7.27
The cyclopentenecarbaldehyde 1a, acetals 2a, 2b and the cyclopentenone 2c have been transformed through regio and stereocontrolled reactions into a variety of enantiomerically pure substituted cyclopentanes. Using appropriately selected Wittig reagents, aldehyde 1a furnished the condensation products 3, 4, 5. Michael addition of diethyl malonate on the α,β-unsaturated aldehyde 1a under phasetransfer
Optically active lactones were synthesized by a novel asymmetric synthesis in which enantiotopic groups remote from a prochiral center were effectively discriminated. The cyclic diamide alcohols bearing a C2-chiral auxiliary, (+)-[1,1'-binaphthyl]-2,2'-diamine (4), were designed and prepared such that the hydroxyl group should attack preferentially at one of the two carbonyl groups. By the catalytic action of trifluoroacetic acid, the substrates 6a,b and 19 were smoothly converted to the lactones 7a (71% de), 7b (97% de), and 20 (> 99% de), the configurations of which were determined to be R, S, and R, respectively. A naturally occurring pheromone, (R)-(+)-5-hexadecanolide (13), was synthesized optically pure from 7b. Transition-state models for the present asymmetric lactonization were constructed according to the stereoelectronic theory proposed by Deslongchamps. The stability of the models was assessed by MM2 calculation, and the direction of asymmetric induction thus calculated coincided with the experimental results.