- Pyridinium N-(2′-azinyl)aminides: Regioselective synthesis of N-(2-pyridyl) substituted polyamines
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The regioselective alkylation of pyridinium-N-(2′-pyridyl)aminide with alkyl dihalides under mild conditions, followed by N-N bond reduction of the corresponding bis-salts, allowed an easy preparation of N,N′-bis(2-pyridyl)diamines. The same methodology h
- José Reyes,Delgado, Francisca,Luisa Izquierdo,Alvarez-Builla, Julio
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- N-Alkylation of poor nucleophilic amines and derivatives with alcohols by a hydrogen autotransfer process catalyzed by copper(II) acetate: Scope and mechanistic considerations
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Copper(II) acetate is a versatile, cheap and simple catalyst for the selective N-monoalkylation of amino derivatives with poor nucleophilic character, such as aromatic and heteroaromatic amines as well as carboxamides, phosphinamides, sulfonamides, and phosphazenes, using in all cases primary alcohols as initial source of the electrophiles, through a hydrogen autotransfer process. In the case of sulfonamides, the monoalkylation process followed by a naphthalene-catalyzed reductive deprotection gives primary amines, which is an indirect alternative to the direct monoalkylation of ammonia. A study of the reaction using deuterium labelled reagents was performed, indicating that the dehydrogenation and hydrogenation steps do not take placed on the same copper-atom coordination sphere, with the condensation step occurring out of the dehydrogenating catalytic species.
- Martínez-Asencio, Ana,Ramón, Diego J.,Yus, Miguel
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experimental part
p. 3140 - 3149
(2011/05/06)
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- Discovery of small molecule CXCR4 antagonists
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In light of a proposed molecular mechanism for the C-X-C chemokine receptor type 4 (CXCR4) antagonist 1 (AMD3100), a template with the general structure 2 was designed, and 15 was identified as a lead by means of an affinity binding assay against the liga
- Zhan, Weiqiang,Liang, Zhongxing,Zhu, Aizhi,Kurtkaya, Serdar,Shim, Hyunsuk,Snyder, James P.,Liotta, Dennis C.
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p. 5655 - 5664
(2008/03/17)
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- CXCR4 ANTAGONISTS FOR THE TREATMENT OF HIV INFECTION
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The invention provides compounds, pharmaceutical compositions and methods of use of certain compounds that are antagonists of the chemokine CXCR4 receptor, and in particular to inhibit viral entry of certain viruses. Certain compounds in particular can reduce entry of immunodeficiency virus (HIV) into a cell while not reducing the capacity of stem cells to proliferate, and therefore can be useful for long term treatment regimes. The compounds are useful in particular in the treatment or prevention of HIV infections.
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Page/Page column 61
(2008/06/13)
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