7743-27-3Relevant academic research and scientific papers
NOVEL CYCLOSPORIN DERIVATIVES AND USES THEREOF
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Paragraph 0242, (2017/12/18)
A compound of the Formula (I) is disclosed: (I) or pharmaceutically acceptable salt thereof, wherein the symbols are as defined in the specification. Also described are a pharmaceutical composition comprising the same and a method for treating or preventing viral infections, inflammation, dry eye, central nervous disorders, cardiovascular diseases, cancer, obesity, diabetes, muscular dystrophy, lung, and liver, and kindey diseases, and hair loss using the same.
Diels-Alder reaction of the dihydropyridinones V: Approach to the ircinal B core
Torisawa, Yasuhiro,Ali, Mohamed Ayman,Tavet, Fabrice,Kageyama, Akiko,Aikawa, Maki,Fukui, Naoko,Hino, Tohru,Nakagawa, Masako
, p. 677 - 689 (2007/10/03)
Thermal and high-pressure Diels-Alder reaction of the suitably assembled dihydropyridinones afforded the hydroisoquinoline derivatives, which were transformed to the key intermediates for the ABC substructure of ircinal B.
Synthesis of pyrrolizidines using aminyl radicals generated from sulfenamide precursors
Russell Bowman,Clark, David N.,Marmon, Robert J.
, p. 1295 - 1310 (2007/10/02)
Tandem radical cyclisations of aminyl radicals generated from sulfenamide precursors have been used for the synthesis of pyrrolizidines and other polycyclic nitrogen heterocycles. The aminyl radicals are generated by reaction between sulfenamide precursor
Synthesis of Chiral Vinylglycines
Beaulieu, Pierre L.,Duceppe, Jean-Simon,Johnson, Carolyne
, p. 4196 - 4204 (2007/10/02)
(R)- or (S)-benzyl 4-formyl-2,2-dimethyl-3-oxazolidinecarboxylate (7a) and (R)- or (S)-1,1-dimethylethyl 4-formyl-2,2-dimethyl-3-oxazolidinecarboxylate (7b), readily available from serine, react with Wittig reagents to give alkenes 8.Selective deprotection followed by oxidation of the resulting unsaturated amino alcohols 9 provides vinylglycines 5 of defined configuration (>95percent ee) and double-bond geometry.D-Vinylglycines are obtained from L-serine, and conversely, D-serine gives β,γ-unsaturated amino acids with the L configuration.The double-bond geometry is controlled by the nature of the phosphorous ylide employed.The scope and limitations of this new methodology for the preparation of chiral vinylglycines is examined.
Synthesis and biological activity of carboxyl-terminus modified prostaglandin analogues
Schaaf,Hess
, p. 1340 - 1346 (2007/10/10)
A series of PGE2, 16,16-dimethyl-PGE2, and PGF(2α), and PGF(2α) analogues modified at the carboxyl terminus with tetrazole, amide, acylurea, imide, and sulfonimide functionalities was evaluated for uterine stimulant, bronchodilator, hypotensive, gastric antisecretory, and diarrheal activity. These compounds were prepared by modification of the Corey prostaglandin synthesis utilizing as a key step condensation of known hemiacetals with the ylide derived from the requisite substituted phosphonium salts. Structure-activity relationships suggest that a proton at the C-1 position appears necessary for agonist activity and the acidity of this proton has a relatively greater influence on activity than pendant steric bulk. Noteworthy are the tissue-selective bronchodilator activity of N-acetyl-PGE2-carboxamide and the selectivity for uterine tissue of N-methanesulfonyl-PGE2-carboxamide, 2-decarboxy-2-(tetrazol-5-yl)-16,16-dimethyl-PGE2, N-acetyl-16,16-dimethyl-PGE2-carboxamide, and N-methanesulfony-PGE2-carboxamide, and N-methanesulfonyl-16,16-dimethyl-PGE2-carboxamide.
