Zobrazeno 1 - 10
of 23
pro vyhledávání: '"Peter J. Lindsay-Scott"'
Autor:
Chuanren Liu, Jing Chen, Ping Huang, John Burnett, Peter J. Lindsay-Scott, Xin Zhang, Jianping Chen, Craig White, John R. Rizzo, Mai Khanh Hawk, Sarah J. Ryan, Yu Lu
Publikováno v:
Organic Process Research & Development. 25:1167-1175
This article describes the use of tetramethylammonium fluoride tetrahydrate (TMAF·4H2O) for the large-scale preparation of a challenging 4-fluorothiazole. Commercially available TMAF·4H2O was procu...
Publikováno v:
Organic Process Research & Development. 24:2853-2863
The synthesis of a subtype-selective inhibitor BACE-1 inhibitor is presented. One of the key transformations in this sequence is the conversion of a thiourea to the bicyclic 1,3-aminooxazine. This ...
Autor:
Hao Sun, Michael O. Frederick, Roger Ryan Rothhaar, Amy C. DeBaillie, Brian Morgan Watson, Carlos Mateos, Leonard L. Winneroski, Carlos Jaramillo, Talbi Kaoudi, Matthew Johnson, Pablo Garcia-Losada, Srinivas Gangula, Peter J. Lindsay-Scott, Steven James Green, Dustin J. Mergott, Dajiang Jing, Marvin M. Hansen, José Eugenio de Diego, Juan A. Rincón, Kevin D. Seibert, Lei Zhang, Jiuyuan Li
Publikováno v:
Organic Process Research & Development. 24:306-314
Herein we report a summary of the synthetic development of LY3202626 from the initial discovery route to a final route that was scaled to make 150 kg. Key developments include the use of a [3 + 2] ...
Publikováno v:
Synthesis. 52:105-118
Synthetic access to 6,7-dihydro-4H-pyrazolo[5,1-c][1,4]oxazines has been achieved in 3–4 steps from commercially available pyrazoles. Optimization of a protected hydroxyethyl group on N1 enabled the regiocontrolled construction of pyrazole-5-aldehy
Publikováno v:
The Journal of Organic Chemistry. 84:13780-13793
Azidoalkyl enol ethers undergo intramolecular 1,3-dipolar cycloaddition to generate stable triazolines; in contrast, the cycloadducts formed by heating analogous azidoalkyl vinyl bromides are unstable with respect to elimination of N2 and HBr, afford
Autor:
Nicolas Dreyfus, James Tseng, Susan Warner, Emily C. Collins, Cristian Constantinescu, Hugh Nuthall, Sergey Shcherbinin, Fanni Natanegara, Roger N. Gunn, Krista M Phipps, Donnelly B. Kevin, Kevin Biglan, Mai Khanh Hawk, Stephen L. Lowe, Susan DuBois, David Russell, J.A. Gilmore, William Kielbasa, Peter J. Lindsay-Scott, Dustin J. Mergott, Xiaoyu Zhang, Nicholas McDonald
Publikováno v:
Alzheimer's & Dementia. 16
Autor:
Peter J. Lindsay-Scott, Victor W. Pike, J. Craig Ruble, Maria Cuadrado, Mohammad B. Haskali, Michael P. Johnson, Susan DuBois, Nancy Kant, Hugh Nuthall, Shuiyu Lu, Jeremy Gilmore, Kevin Michael Ruley, Aneta Kowalski, Enrique Jambrina, S Michelle Morin, Adrian J. Mogg, Soumen Paul, Andrew J. Mannes, Jeih-San Liow, Vanessa N. Barth, Cheryl L. Morse, Sami S. Zoghbi, Nicolas Dreyfus, Robert L. Gladding, Cynthia Darshini Jesudason, Robert B. Innis, Sergey Shcherbinin
Publikováno v:
Science Translational Medicine. 12
We aimed to develop effective radioligands for quantifying brain O-linked-β-N-acetyl-glucosamine (O-GlcNAc) hydrolase (OGA) using positron emission tomography in living subjects as tools for evaluating drug target engagement. Posttranslational modif
Autor:
Alexandru Grozavu, Timothy J. Donohoe, Hamish B. Hepburn, Peter J. Lindsay-Scott, Elliot P. Bailey
Publikováno v:
Chemical Science
Pyridines are ubiquitous aromatic rings used in organic chemistry and are crucial elements of the drug discovery process. Herein we describe a new catalytic method that directly introduces a methyl group onto the aromatic ring; this new reaction is r
Publikováno v:
The Journal of Organic Chemistry. 82:11295-11303
A four-step protocol for the synthesis of pyrazolo[1,5-a]pyrazines has been developed. Commercially available pyrazoles were alkylated and formylated in a regiocontrolled manner to give pyrazole-5-aldehydes bearing 2,2-dialkoxyethyl substitution on N
Publikováno v:
Tetrahedron Letters. 58:2629-2635
Arylacetonitriles are versatile building blocks for the construction of heterocyclic scaffolds in medicinal chemistry. These intermediates are able to engage in a variety of synthetic transformations, giving rise to diverse biologically active struct