162541-45-9Relevant academic research and scientific papers
PYRAZOLOPYRAZINES AND THEIR USE IN THE TREATMENT, AMELIORATION OR PREVENTION OF A VIRAL DISEASE
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Page/Page column 42; 43, (2017/04/11)
The present invention relates to a compound having the general formula (IIa) or (IIb), optionally in the form of a pharmaceutically acceptable salt, solvate, polymorph,codrug, cocrystal,prodrug, tautomer, racemate, enantiomer, or diastereomer or mixture thereof, which are useful in treating, ameloriating or preventing a viral disease. Furthermore, specific combination therapies are disclosed.
Nickel-catalyzed regiodivergent opening of epoxides with aryl halides: Co-catalysis controls regioselectivity
Zhao, Yang,Weix, Daniel J.
supporting information, p. 48 - 51 (2014/01/23)
Epoxides are versatile intermediates in organic synthesis, but have rarely been employed in cross-coupling reactions. We report that bipyridine-ligated nickel can mediate the addition of functionalized aryl halides, a vinyl halide, and a vinyl triflate to epoxides under reducing conditions. For terminal epoxides, the regioselectivity of the reaction depends upon the cocatalyst employed. Iodide cocatalysis results in opening at the less hindered position via an iodohydrin intermediate. Titanocene cocatalysis results in opening at the more hindered position, presumably via TiIII-mediated radical generation. 1,2-Disubstituted epoxides are opened under both conditions to form predominantly the trans product.
METHOD OF PRODUCING PYRONE AND PYRIDONE DERIVATIVES
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Page/Page column 36-37, (2012/02/03)
The present invention provides a pyrone derivative and a pyridone derivative, which are novel intermediates for synthesizing an anti-influenza drug, a method of producing the same, and a method of using the same.
INHIBITORS OF AKT ACTIVITY
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Page/Page column 35, (2008/12/08)
Invented are novel heterocyclic carboxamide compounds, the use of such compounds as inhibitors of protein kinase B activity and in the treatment of cancer and arthritis.
INHIBITORS OF AKT ACTIVITY
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Page/Page column 40, (2008/12/04)
Invented are novel pyrazole compounds, the use of such compounds as inhibitors of protein kinase B activity and in the treatment of cancer and arthritis.
Synthesis of Peptidosulfinamides and Peptidosulfonamides: Peptidomimetics Containing the Sulfinamide or Sulfonamide Transition-State Isostere
Moree, Wilna J.,Marel, Gijs A. van der,Liskamp, Rob J.
, p. 5157 - 5169 (2007/10/02)
Synthetic routes are described toward the preparation of α- as well as β-substituted aminoethanesulfinyl chlorides, starting from either an aldehyde or from an amino acid derivative.The sulfinyl chlorides are used as building blocks for the preparation of homochiral α- or β-substituted sulfinamide and sulfonamide transition-state isosteres.The methodology has been applied to the synthesis of peptidosulfonamide peptidomimetics such as a hapten needed for the generation of antibodies and potential HIV protease inhibitors.In addition, the β-substituted aminoethanesulfinyl chlorides were used as building blocks for the preparation of a tetrapeptidosulfonamide, which can be considered as a biopolymer mimetic, employing a repetition of a cycle of three reactions: coupling of the sulfinyl chloride to the N-terminus of the growing peptidosulfonamide, oxidation to the sulfonamide, and deprotection of the N-terminus.
