251948-87-5Relevant academic research and scientific papers
A versatile polypeptoid platform based on N-allyl glycine
Robinson, Joshua W.,Schlaad, Helmut
, p. 7835 - 7837 (2012)
N-Allyl glycine N-carboxyanhydride (NCA) was synthesized and polymerized by ring opening polymerization under homo- or heterophase conditions to afford well-defined polypeptoids (MW = 1.5-10.5 kg mol-1, PDI = 1.1-1.4). Poly(N-allyl glycine) demonstrated stimuli-responsive behaviour in water and was readily modified via thiol-ene photochemistry under experimentally benign conditions. This journal is
Discovery and Early Clinical Development of LY3202626, a Low-Dose, CNS-Penetrant BACE Inhibitor
McKinzie, David L.,Winneroski, Leonard L.,Green, Steven J.,Hembre, Erik J.,Erickson, Jon A.,Willis, Brian A.,Monk, Scott A.,Aluise, Christopher D.,Baker, Thomas K.,Lopez, Jose E.,Hendle, J?rg,Beck, James P.,Brier, Richard A.,Boggs, Leonard N.,Borders, Anthony R.,Cocke, Patrick J.,Garcia-Losada, Pablo,Lowe, Stephen L.,Mathes, Brian M.,May, Patrick C.,Porter, Warren J.,Stout, Stephanie L.,Timm, David E.,Watson, Brian M.,Yang, Zhixiang,Mergott, Dustin J.
, p. 8076 - 8100 (2021/06/28)
The beta-site APP cleaving enzyme 1, known as BACE1, has been a widely pursued Alzheimer's disease drug target owing to its critical role in the production of amyloid-beta. We have previously reported the clinical development of LY2811376 and LY2886721. L
TRICYCLIC INHIBITORS OF HEPATITIS B VIRUS
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Page/Page column 53, (2020/03/02)
The present invention relates to compounds that are inhibitors of hepatitis B virus (HBV). Compounds of this invention are useful alone or in combination with other agents for treating, ameliorating, preventing or curing HBV infection and related conditions. The present invention also relates to pharmaceutical compositions containing said compounds.
BACE INHIBITORS
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Page/Page column 20-21, (2014/05/24)
The present invention provides compounds of Formula I useful as BACE inhibitors in the treatment of e.g. Alzheimer's disease : wherein A is selected from the group consisting of; of; R1 is H or F; R2 is H, -OCH3, C1-C3 alkyl,; R3 is H, -CH3, or -OCH3; and R4 is H or F; or a pharmaceutically acceptable salt thereof.
Easy and efficient generation of reactive anions with free and supported ylides as neutral Bronsted bases
Palacios, Francisco,Aparicio, Domitila,De Los Santos, Jesús M.,Baceiredo, Antoine,Bertrand, Guy
, p. 663 - 669 (2007/10/03)
The tris(dimethylamino)-C-dimethylphosphorus ylide 5 and the tris(dimethylamino)phosphorus ylide C-bound to Merrifield's resin 6 are used as strong non-nucleophilic bases in N-alkylation reactions of β-amino phosphine oxides and α-amino acid derivatives,
Pd-catalyzed asymmetric allylic alkylation of 3-acetoxy-N-(tert- butyloxycarbonyl)-1,2,3,6-tetrahydropyridine - Preparation of key intermediates for natural product synthesis
Schleich, Simone,Helmchen, Guenter
, p. 2515 - 2521 (2007/10/03)
A convenient synthesis of racemic tetrahydropyridine 1 was developed. Pd-catalyzed allylic alkylation of 1 with malonate and dimethylacetoxymalonate as nucleophiles with the phosphanylcarboxylic acid L1 and the dihydrooxazol L2 as ligands, were carried out and gave enantiomeric excesses of up to 98%. Absolute configurations were determined for all compounds described. From the alkylation products (+)- and (-)-2a, and (+)- and (-)-2b a variety of versatile, nonracemic chiral intermediates were prepared.
