105960-29-0Relevant articles and documents
PRODRUGS OF FUSED-BICYCLIC C5aR ANTAGONISTS
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Paragraph 0248, (2019/10/23)
The present disclosure provides, inter alia, Compounds of Formulae IA, IB, IC, IIA, IIB and IIC or pharmaceutically acceptable salts thereof that are modulators of the C5a receptor. Also provided are pharmaceutical compositions and methods of use including the treatment of diseases or disorders involving pathologic activation from C5a and non-pharmaceutical applications.
Phenolic Oxidation Using H2O2 via in Situ Generated para-Quinone Methides for the Preparation of para-Spiroepoxydienones
McLaughlin, Michael F.,Massolo, Elisabetta,Cope, Thomas A.,Johnson, Jeffrey S.
supporting information, p. 6504 - 6507 (2019/09/04)
Phenols are attractive starting materials for the preparation of highly substituted cyclohexane rings via dearomative processes. Herein we report an efficient preparation of dearomatized 1-oxaspiro[2.5]octa-4,7-dien-6-ones (para-spiroepoxydienones) via the nucleophilic epoxidation of in situ generated para-quinone methides from 4-(hydroxymethyl)phenols using aqueous H2O2. The developed protocol bypasses the need for stoichiometric bismuth reagents or diazomethane, which are frequently deployed for p-spiroepoxydienone preparation. The p-spiroepoxydienones are further elaborated in numerous downstream complexity-building transformations.
AROMATASE INHIBITOR
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Page/Page column 87, (2011/04/14)
There is provided a compound of formula (I) wherein Z is selected from N and CR22, wherein R22 is H or a bond with D, wherein D is selected from a bond, C=O, and linear or branched hydrocarbon groups having a carbon chain of from 1 t
Prodrugs of anthracyclines for use in antibody-directed enzyme prodrug therapy
Florent, Jean-Claude,Dong, Xia,Gaudel, Gilbert,Mitaku, Sofia,Monneret, Claude,Gesson, Jean-Pierre,Jacquesy, Jean-Claude,Mondon, Martine,Renoux, Brigitte,Andrianomenjanahary, Solo,Michel, Sylvie,Koch, Michel,Tillequin, Fran?ois,Gerken, Manfred,Czech, Joerg,Straub, Rainer,Bosslet, Klaus
, p. 3572 - 3581 (2007/10/03)
A series of new prodrugs of daunorubicin and doxorubicin which are candidates for antibody-directed enzyme prodrug therapy (ADEPT) is reported. These compounds (25a,b,c and 32a,b,c) have been designed to generate cytotoxic drugs after activation with β-gl
Acetals as New 2′-O-Protecting Functions for the Synthesis of Oligoribonucleotides: Synthesis of Uridine Building Blocks and Evaluation of Their Relative Acid Stability
Matysiak, Stefan,Fitznar, Hans-Peter,Schnell, Ralf,Pfleiderer, Wolfgang
, p. 1545 - 1566 (2007/10/03)
A broad variety of new acyclic vinyl ethers (see 6-41) have been synthesized via the vinyl-interchange reaction of ethyl vinyl ether at room temperature using mercury(II) trifluoroacetate as a highly efficient catalyst. The appropriate vinyl ethers were r
Biologically Active Metabolites of Fungi, I.-Isolation, Synthesis, and Biological Activity of Coniothyriomycin as well as Bioassay of Analogous Open-Chain Imides
Krohn, Karsten,Franke, Claudia,Jones, Peter G.,Aust, Hans-Juergen,Draeger, Sigfried,Schulz, Barbara
, p. 789 - 798 (2007/10/02)
The mixed open-chain imide N-(3-chloro-4-hydroxyphenylacetyl)fumarate (1), named coniothyriomycin, was isolated as a metabolite of the fungus Coniothyrium.The natural product 1 and the analoguos imides 13-15 and 22-24 have been synthesized by base-catalyzed condensation of the imidates 12a-f with acid chlorides 6a-c or the mixed anhydride 21.The compounds 1 and 13-15 were shown to posess remarkable fungicidal and herbicidal activities in short-termed tests. Key Words: Fungal metabolites / Imides, open-chain / Fungicidal activity / Coniothriomycin