612494-07-2Relevant academic research and scientific papers
Evaluation of a 4-aminopiperidine replacement in several series of CCR5 antagonists
Lemoine, Rémy C.,Petersen, Ann C.,Setti, Lina,Chen, Lijing,Wanner, Jutta,Jekle, Andreas,Heilek, Gabrielle,deRosier, André,Ji, Changhua,Rotstein, David M.
scheme or table, p. 1830 - 1833 (2010/07/02)
The bicyclic 5-amino-3-azabicyclo[3.3.0]octanes were shown to be effective replacements for the conformationally restricted 4-aminopiperidine ring found in several series of CCR5 antagonists.
Piperazine-Based CCR5 Antagonists as HIV-1 Inhibitors. IV. Discovery of 1-[(4,6-Dimethyl-5-pyrimidinyl) carbonyl]-4-[4-{2-methoxy-1(R)-4-(trifluoromethyl)-phenyl}ethyl-3(S) -methyl-1-piperazinyl]-4-methylpiperidine (Sch-417690/Sch-D), a Potent, Highly Sel
Tagat, Jayaram R.,McCombie, Stuart W.,Nazareno, Dennis,Labroli, Marc A.,Xiao, Yushi,Steensma, Ruo W.,Strizki, Julie M.,Baroudy, Bahige M.,Cox, Kathleen,Lachowicz, Jean,Varty, Geoffrey,Watkins, Robert
, p. 2405 - 2408 (2007/10/03)
The nature and the size of the benzylic substituent are shown to be the key to controlling receptor selectivity (CCR5 vs M1, M2) and potency in the title compounds. Optimization of the lead benzylic methyl compound 3 led to the methoxymethyl analogue 30,
Stereoselective alkylation of chiral 2-methyl-4-protected piperazines
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Page/Page column 11, (2008/06/13)
In an illustrative embodiment, the present invention describes the synthesis of the following compound and similar compounds, in high stereochemical purity by a novel stereoselective alkylation process: 1
