182352-48-3Relevant academic research and scientific papers
Efficient total synthesis of pulchellalactam, a CD45 protein tyrosine phosphatase inhibitor
Li, Wen-Ren,Lin, Sung Tsai,Hsu, Nai-Mu,Chern, Meei-Shiou
, p. 4702 - 4706 (2002)
A new approach to a CD45 protein tyrosine phosphatase inhibitor, pulchellalactam, is described. The key step of the sequence involves addition and elimination of an enolic lactam in a single step and 70% yield, employing an organocuprate reagent. The resulting α,β-unsaturated lactam could be condensed with isobutyraldehyde to produce Z-pulchellalactam or converted into siloxypyrrole, which was subjected to the BF3·Et2O-promoted coupling reaction with isobutyraldehyde to afford E-pulchellalactam after E1-cB elimination and TFA deprotection. This first total synthesis afforded Z-pulchellalactam in six steps and 32% overall yield from Boc-glycine. The same sequence of reactions could also be applied to the liquid- or solid-phase synthesis of trifunctionalized pulchellalactam derivatives.
Short synthesis of 4-aryl-3-pyrrolin-2-ones
Yoon-Miller, Sarah J.P.,Opalka, Suzanne M.,Pelkey, Erin T.
, p. 827 - 830 (2007)
A three step, convergent synthesis of 4-aryl-3-pyrrolin-2-ones from a tetramic acid has been developed. The key transformation utilized a Suzuki-Miyaura cross-coupling reaction between a 4-tosyloxy-3-pyrrolin-2-one and an arylboronic acid. This work also
COMPOUNDS FOR USE IN TREATING NEUROLOGICAL DISORDERS
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Paragraph 00178-00179, (2021/02/05)
Provided are methods for treating neurological disorders using compounds of Formula (I), and pharmaceutically acceptable salts and compositions thereof.
METHODS AND COMPOSITIONS FOR MODULATING SPLICING
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, (2020/08/22)
Described herein are small molecule splicing modulator compounds that modulate splicing of mRNA, such as pre-mRNA, encoded by genes, and methods of use of the small molecule splicing modulator compounds for modulating splicing and treating diseases and conditions.
P300/CBP HAT INHIBITORS
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Paragraph 00110; 00194-00195, (2019/09/04)
Provided are compounds of Formula (I): and pharmaceutically acceptable salts and compositions thereof, which are useful for treating a variety of conditions associated with histone acetyltransferase (HAT).
TYK2 INHIBITORS AND USES THEREOF
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Paragraph 001028-001029, (2017/03/21)
The present invention provides compounds, compositions thereof, and methods of using the same for the inhibition of TYK2, and the treatment of TYK2-mediated disorders.
Aminoheteroaryl benzamides as kinase inhibitors
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Page/Page column 397; 398; 399, (2016/02/15)
The present invention provides a compound of Formula (I) or a salt thereof; and therapeutic uses of these compounds. The present invention further provides pharmaceutical compositions comprising these compounds, and compositions comprising these compounds with a therapeutic co-agent.
TAMBJAMINES AND B-RING FUNCTIONALIZED PRODIGININES
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Page/Page column 17; 18; 26, (2016/11/17)
Embodiments of tambjamines and B-ring functionalized prodiginines are disclosed. Methods of synthesizing and using the disclosed compounds are also disclosed. Some embodiments of the disclosed compounds have antimalarial activity. Certain embodiments of t
Synthesis and Structure-Activity Relationships of Tambjamines and B-Ring Functionalized Prodiginines as Potent Antimalarials
Kancharla, Papireddy,Kelly, Jane Xu,Reynolds, Kevin A.
, p. 7286 - 7309 (2015/10/05)
Synthesis and antimalarial activity of 94 novel bipyrrole tambjamines (TAs) and a library of B-ring functionalized tripyrrole prodiginines (PGs) against a panel of Plasmodium falciparum strains are described. The activity and structure-activity relationsh
Synthesis of fluorinated tricyclic scaffolds by intramolecular [2+2] photocycloaddition reactions
Fort, Diego A.,Woltering, Thomas J.,Nettekoven, Matthias,Knust, Henner,Bach, Thorsten
supporting information, p. 10169 - 10172 (2012/11/07)
Fabulous Fluorine: The synthesis of fluorinated products 1 and 2 by [2+2] photocycloaddition was readily feasible after optimization of the irradiation conditions. The electron-deficient trifluoroolefin unit reacted intramolecularly to products 1 (nine ex
