NOVEL THIOPHENE DERIVATIVES AS S1P1/EDG1 RECEPTOR AGONISTS
The invention relates to thiophene derivatives of formula (I) / their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunosuppressive agents wherein: A represents *-CO-CH=CH-, *-CO-CH2CH2-, *-CO-CH2-NH-, wherein the sterisks indicate the bond that is linked to the thiophene group of Formula (I) , and R1-R3 are as defined in the claims.
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Page/Page column 36
(2010/11/28)
The Willgerodt-Kindler Reactions. 6. Isomerization of the Carbonyl Group in Alkanones and Cycloalkanones
The most unusual feature of the Willgerodt-Kindler Reactions is the facile isomerization of the carbonyl function along a chain of unbranched methylene groups, or around a cycloaliphatic ring containing several connected methylene groups.We have demonstrated that the first step in the Kindler process is the formation of enamines by reaction of the carbonyl function with secondary aliphatic amines, followed by reaction of the enamine with certain sulfur-amine catalysts to form reactive heterocyclic sulfur intermediates that facilitate the elimination-readdition of the amines reversibly along the chain.It was shown that compounds of the type R2N-S-S-NR2 are effective catalysts but not compounds of the type R2N-S-NR2.Some cyclohexanone derivatives undergo aromatization, with anomalous results in certain cases.
Carmack, Marvin,Behforouz, Mohammad,Berchtold, Glenn A.,Berkowitz, Samuel M.,Wiesler, Donald,Barone, Ralph
p. 1305 - 1318
(2007/10/02)
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