3842-86-2Relevant academic research and scientific papers
TRANSGLUTAMINASE 2 (TG2) INHIBITORS
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Paragraph 00282, (2020/03/02)
Described herein are compounds and pharmaceutical compositions containing such compounds which inhibit transglutaminase 2 (TG2). Also described herein are methods for using such TG2 inhibitors, alone or in combination with other compounds, for treating diseases or conditions that would benefit from TG2 inhibition.
METHODS AND INTERMEDIATES FOR THE PREPARATION OF MACROLACTAMS
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Page/Page column 55, (2015/07/07)
The present invention relates to synthetic processes useful in the preparation of macrolactams that inhibit hepatitis C virus (HCV), specifically macrolactam compounds that inhibit the HCV NS3 protease activity and have application in the treatment of conditions caused by HCV. The present invention also encompasses intermediates useful in the disclosed synthetic processes and the methods of their preparation.
Sanglifehrin based compounds
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Page/Page column 70; 71; 72, (2015/09/23)
There are provided inter alia compounds of formula (I) useful as cyclophilin inhibitors.
Deprotonation of β,β-disubstituted α,β-unsaturated amides -Mechanism and stereochemical consequences
Green, James R.,Majewski, Marek,Snieckus, Victor
, p. 1397 - 1410 (2007/10/03)
A detailed study of the lithium dialkylamide induced deprotonation of β,β-disubstituted α,β-unsaturated amides is presented. The preferential γ-Z-deprotonation and stereochemical outcome of substituents on the γ-Z carbon atom are rationalized in terms of a cyclic eight-membered transition state, which is supported by DFT calculations. Analogous deprotonations on cyclohexylidenecarboxamides reveal a delicate balance of the preference for the eight-membered cyclic transition state with the effects of existing substituents on the ring and the intervention of a twist-boat transition state.
PHOSPHONATES α-LITHIES, AGENTS DE TRANSFERT FONCTIONNEL. PREPARATION DE PHOSPHONATES α-AMIDES ET D'AMIDES α,β-INSATURES, α-SUBSTITUES
Tay, M.K.,About-Jaudet, E.,Collignon, N.,Savignac, P.
, p. 4415 - 4430 (2007/10/02)
Lithiated anions (9) or (10) of secondary or tertiary α-amidophosphonates are prepared either by reaction between an α-phosphonyl carbanion and an isocyanate or a carbamate (first strategy), or by condensation of an amide enolate with diethylchlorophosphate (second strategy).Acidic hydrolysis of (9) or (10) gives α-amidophosphonate (1) alkylated or not in the α-position. (9) and (10) react with aromatic or aliphatic aldehydes to produce α,β-unsatured secondary or tertiary amides (2).
PREPARATION QUASI QUANTITATIVE DE PHOSPHONATES β-CARBONYLES PAR L'EMPLOI D'UNE BASE RELAIS, LE DIPAL
Aboujaoude, Elie Elia,Collignon, Noel,Teulade, Marie-Paule,Savignac, Philippe
, p. 57 - 62 (2007/10/02)
Preparation of oxo-2 alkylphosphonates by anionic route is a process of limited scope.The low yields often encountered in the initial phosphonylation step are certainly due to regeneration of the departure phosphonate through acid-base exchanges.This drawback can be overcome by proper choice of the metalating agent.The use of LDA makes the procedure efficient and most stoechiometric, and it lends itself to the preparation of a wide range of β-ketophosphonates free of by-products.
