7151-64-6Relevant articles and documents
CONTROLLED DRUG RELEASE FROM SOLID SUPPORTS
-
Page/Page column 31-32, (2011/11/30)
The invention relates to solid supports useful in medical applications that provide controlled release of drugs, such as peptides, nucleic acids and small molecules. The drugs are covalently coupled to the solid support through a linkage that releases the drug or a prodrug through controlled beta elimination.
Reactions of diazo compounds with alkenes catalysed by [RuCl(cod)(Cp)]: Effect of the substituents in the formation of cyclopropanation or metathesis products
Basato, Marino,Tubaro, Cristina,Biffis, Andrea,Bonato, Marco,Buscemi, Gabriella,Lighezzolo, Filippo,Lunardi, Pamela,Yianini, Chiara,Benetollo, Franco,Del Zotto, Alessandro
experimental part, p. 1516 - 1526 (2009/09/04)
The reaction of diazo compounds with alkenes catalysed by complex [RuCl(COd)(Cp)] (cod = 1, 5-cyclooctadiene, Cp = cyclopentadienyl) has been studied. The catalytic cycle involves in the first step the decomposition of the diazo derivative to afford the reactive [RuCl(Cp)I=C(R1)R 2)] intermediate and a mechanism is proposed for this step based on a kinetic study of the simple coupling reaction of ethyl diazoacetate. The evolution of the Ru-carbene intermediate in the presence of alkenes depends on the nature of the substituents at both the diazo N2=C(R 1)R2 (R1, R2 = Ph, H; Ph, CO 2Me; Ph, Ph; C(R1)R2 = fluorene) and the olefin substrates R3(H)C= C(H)R4 (R3, R4 = CO2Et, CO2Et; Ph, Ph; Ph, Me; Ph, H; Me, Br; Me, CN; Ph, CN; H, CN; CN, CN). A remarkable reactivity of the complex was recorded, especially towards unstable aryldiazo compounds and electron-poor olefins. The results obtained indicate that either cyclopropanation or metathesis products can be formed: the first products are favoured by the presence of a cyano substituent at the double bond and the second ones by a phenyl.
Diels-Alder Reaction: 1,4-Cycloaddition of N-Aryl-maleimides to Alkylidene- and Arylidene-fluorenones and Synthesis of Some New Fluoranthene Derivatives
Abdou, Sadek E.,Habashy, Adiba,Aziz, Gamil,Khalifa, Fathy
, p. 755 - 758 (2007/10/02)
The 1,4-cycloaddition of different N-arylmaleimides (IIa-f) to alkylidene- and arylidene-fluorenones (Ia-c) leads to the formation of the diadducts, 7-substituted-5-aryl-4,6-dioxo-4H-3,3a,5,6,6a,7,10b-octahydrofluoranthenopyrrole-endo(3,10b)-N-arylpyrrolidino-2',5'-diones (IIIa-r).The fully aromatized fluoranthene derivatives (Va-i) have also been synthesised either by boiling III in nitrobenzene or by reacting the bromo-derivatives (V) with appropriate II.Reduction of III using LAH gives VIII.The structures of the isolated products have been confirmed by elemental analyses, molecular weight determination and spectroscopic data.