6727-73-7Relevant academic research and scientific papers
NOVEL ANTIVIRAL PYRROLOPYRIDINE DERIVATIVES AND METHOD FOR PREPARING THE SAME
-
Paragraph 0431; 0432; 0433, (2014/09/16)
The present invention relates to a pyrrolopyridine derivative represented by the Chemical Formula I, and a racemate or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof, and relates to an antiviral composition including the same as an active ingredient. The compound of the Chemical Formula I has excellent antiviral activity and selectivity for wild type and resistant HIV-1, and thereby is useful as a therapeutic agent for acquired immune deficiency syndrome (AIDS).
NOVEL ANTIVIRAL PYRROLOPYRIDINE DERIVATIVE AND A PRODUCTION METHOD FOR SAME
-
Paragraph 0412; 0413; 0414, (2014/12/09)
The present invention relates to a pyrrolopyridine derivative represented by the Chemical Formula I, and a racemate or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof, and relates to an antiviral composition including the same as an active ingredient. The compound of the Chemical Formula I has excellent antiviral activity and selectivity for wild type and resistant HIV-1, and thereby is useful as a therapeutic agent for acquired immune deficiency syndrome (AIDS).
A new sequential intramolecular cyclization based on the boekelheide rearrangement
Massaro, Assunta,Mordini, Alessandro,Mingardi, Anna,Klein, Jens,Andreotti, Daniele
supporting information; experimental part, p. 271 - 279 (2011/02/28)
Pyrrolidines and piperidines were synthesized from (aminoalkyl)pyridine N-oxides with a general and quite efficient method developed by using di-tert-butylsilyl bis(trifluoromethanesulfonate) as a new promoter for a Boekelheide-type reaction. The use of a
Nickel-catalyzed rearrangement of 1-acyl-2-vinylcyclopropanes. A mild synthesis of substituted dihydrofurans
Bowman, Roy K.,Johnson, Jeffrey S.
, p. 573 - 576 (2007/10/03)
Mild Ni(0)-catalyzed rearrangements of 1-acyl-2-vinylcyclopropanes have been developed. The room-temperature isomerizations afford dihydrofuran products in yields regularly greater than 90%. A highly substituted, stereochemically defined cyclopropane was
Zn-promoted regioselective and sequence-selective one-pot joining reaction of three components: Alkyl iodides, α,β-unsaturated esters (or nitriles), and acylating agents
Yamamoto, Yoshimasa,Nakano, Seiji,Maekawa, Hirofumi,Nishiguchi, Ikuzo
, p. 799 - 802 (2007/10/03)
One-pot treatment of alkyl iodides, α,β-unsaturated esters (or nitriles), and acylating agents such as nitriles or acid anhydrides in the presence of Zn metal at room temperature in the same reaction system brought about a regioselective and sequence-selective three-component joining reaction involving first C-alkylation at the β-position and second C-acylation at the α-position of α,β-unsaturated esters (or nitriles) to afford the corresponding α,α-dialkylketoesters (or α,α-dialkylketonitriles) in moderate to good yields.
Nickel-catalyzed cross-couplings of organosilicon reagents with unactivated secondary alkyl bromides
Powell, David A.,Fu, Gregory C.
, p. 7788 - 7789 (2007/10/03)
A metal-catalyzed cross-coupling of organosilicon compounds with alkyl halides has been developed. Noteworthy attributes of the method are its scope (secondary electrophiles), its high functional-group compatibility, and the air stability of the catalyst components. Copyright
Unsymmetrical Ketone Synthesis via a Three-Component Connection Reaction of Organozincs, Allylating Agents, and Carbon Monoxide
Yasui, Kengo,Fugami, Keigo,Tanaka, Shuji,Tamaru, Yoshinao
, p. 1365 - 1380 (2007/10/02)
A wide variety of organozincs (diethylzinc, alkylzinc halides, and organozincs 2, 5, and 9a-e, functionalized with ester and nitrile groups) undergo a three-component connection reaction with carbon monoxide and allylic benzoates or phosphates 1a-h to furnish unsymmetrical ketones, e.g., 3, 6, and 10, in good yields uder 1 atm of carbon monoxide at ambient temperature by the catalysis of tetrakis(triphenylphosphine)palladium in THF/HMPA.The regio- and stereoselectivities of the present carbonylation show marked contrast to those reported for the palladium-catalyzed carbonylation of usymmetrical allylic substrates.For example, the reaction of crotyl benzoate with octylzinc iodide provides all the possible stereo- and regioisomers, i.e., cis- and trans-2-butenyl and 1-methyl-2-propenyl octyl ketones in comparable amounts.The carbonylative coupling of carvyl phosphates, trans- and cis-1h, and γ-zincio ester 5 is stereospecific and proceeds with inversion of configuration at the allylic stereocenters to furnish cis- and trans-6h, respectively, as single diastereomers.In the absence of HMPA, the reaction feature changes dramatically and lactones 12 and 13 (composed of organozincs, carbon monoxide, and allylating agents in the ratios of 1:1:2 and 2:1:1, respectively) and symmetrical keto diesters 14 (composed of 2 mol of organozincs and 1 mol of carbon monoxide) are formed in varying ratios depending on the reaction conditions.Synthetic scope of the unsymmetrical ketones and mechanistic rationale for these unique and unprecedented reaction behaviors are discussed.
