126788-88-3Relevant academic research and scientific papers
SUBSTITUTED PYRAZOLOAZEPIN-8-ONES AND THEIR USE AS PHOSPHODIESTERASE INHIBITORS
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Page/Page column 44, (2018/07/05)
The present invention relates to novel pyrazoloazepin-8-ones with phosphodiesterase inhibitory activity, as well as to their use as therapeutic agents in the treatment of inflammatory diseases and conditions.
Probing the influence of an allylic methyl group in zearalenone analogues on binding to Hsp90
Rink, Christian,Sasse, Florenz,Zubrienae -, Asta,Matulis, Daumantas,Maier, Martin E.
supporting information; experimental part, p. 14469 - 14478 (2011/03/21)
By the replacement of an acetate with propionate by means of organic synthesis, a range of zearalenone analogues were prepared that feature an allylic methyl group. For the synthesis of the aliphatic region of the analogues, we used an asymmetric alkylati
Highly enantioselective synthesis of atropisomeric anilide derivatives through catalytic asymmetric N-arylation: Conformational analysis and application to asymmetric enolate chemistry
Kitagawa, Osamu,Yoshikawa, Masatoshi,Tanabe, Hajime,Morita, Tomofumi,Takahashi, Masashi,Dobashi, Yasuo,Taguchi, Takeo
, p. 12923 - 12931 (2008/02/05)
In the presence of (R)-DTBM-SEGPHOS-Pd(OAc)2 catalyst, N-arylation (aromatic amination) of various o-tert-butylanilides with p-iodonitrobenzene proceeds with high enantioselectivity (88-96% ee) to give atropisomeric N-(p-nitrophenyl)anilides having an N-C chiral axis in good yields. Atropisomeric anilide products highly prefer to exist as the E-rotamer which has trans-disposed o-tert-butylphenyl group and carbonyl oxygen. The application of the present catalytic enantioselective N-arylation to an intramolecular version gives atropisomeric lactam derivatives with high optical purity (92-98% ee). The reaction of the lithium enolate prepared from the atropisomeric anilide and lactam products with various alkyl halides gives α-alkylated products with high diastereoselectivity (diastereomer ratio = 13:1 to 46:1).
A stereoselective synthesis of (2S,4R)-δ-hydroxyleucine methyl ester: A component of cyclomarin A
Hansen, Darren B.,Starr, Mari-Lynn,Tolstoy, Nikolai,Joullie, Madeleine M.
, p. 3623 - 3627 (2007/10/03)
(2S,4R)-δ-Hydroxyleucine methyl ester, the N-demethyl analogue of an amino acid contained within the macrocycle of cyclomarin A, was successfully synthesized using Davis' asymmetric Strecker reaction.
Chemistry of tricarbonyl hemiketals and application of Evans' technology to the total synthesis of the immunosuppressant (-)-FK-506
Jones,Reamer,Desmond,Mills
, p. 2998 - 3017 (2007/10/02)
Details of model studies probing the chemistry of the tricarbonyl region of FK-506 are presented, and their use in designing a successful route to this immunosuppressant is outlined. Application of asymmetric oxazolidinone alkylation/aldol methodology to a convergent, highly flexible synthesis of the C10-C18 fragment and to improvements in the preparation of the C20-C34 segment are also discussed.
