- METHOD FOR PRODUCING PRIMARY AMINES
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PROBLEM TO BE SOLVED: To provide a method for producing primary amines industrially, economically, safely, and efficiently. SOLUTION: Provided is a method for producing primary amines represented by R1-NH2 by reacting, in the presence of an acid catalyst, an imine compound, represented by formula (1), and an alcohol represented by R4-(OH)n, comprising a step of distilling off the primary amine from a reaction mixture which is in the reaction process. (R1 is an alkyl group or an alkenyl group; R2 is H, an alkyl group, or an aryl group; R3 is an aryl group; R4 is an n-valent hydrocarbon roup; and n is an integer of 1 to 3.) SELECTED DRAWING: None COPYRIGHT: (C)2019,JPOandINPIT
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Paragraph 0047; 0048
(2019/08/27)
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- Poly(phosphorodiamidate)s by Olefin Metathesis Polymerization with Precise Degradation
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Degradable polymers are a currently growing field of research for biomedical and materials science applications. The majority of such compounds are based on polyesters and polyamides. In contrast, their phosphorus-containing counterparts are much less studied, in spite of their potential precise degradation profile and biocompatibility. Herein, the first library of poly(phosphorodiamidate)s (PPDAs) with two P?N bonds forming the polymer backbone and a pendant P?OR group is prepared through acyclic diene metathesis polymerization. They are designed to vary in their hydrophilicity and are compared with the structural analogues poly(phosphoester)s (PPEs) with respect to their thermal properties and degradation profiles. The degradation of PPDAs can be controlled precisely by the pH: under acidic conditions the P?N linkages in the polymer backbone are cleaved, whereas under basic conditions the pendant ester is cleaved selectively and almost no backbone degradation occurs. The PPDAs exhibit distinctively higher thermal stability (from thermogravimetric analysis (TGA)) and higher glass transition and/or melting temperatures (from differential scanning calorimetry (DSC)) compared with analogous PPEs. This renders this exotic class of phosphorus-containing polymers as highly promising for the development of future drug carriers or tissue engineering scaffolds.
- Steinmann, Mark,Wagner, Manfred,Wurm, Frederik R.
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p. 17329 - 17338
(2016/11/23)
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- Macrocyclic inhibitors of the malarial aspartic proteases plasmepsin I, II, and IV
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The first macrocyclic inhibitor of the Plasmodium falciparum aspartic proteases plasmepsin I, II, and IV with considerable selectivity over the human aspartic protease cathepsin D has been identified. A series of macrocyclic compounds were designed and synthesized. Cyclizations were accomplished using ring-closing metathesis with the second generation Grubbs catalyst. These compounds contain either a 13-membered or a 16-membered macrocycle and incorporate a 1,2-dihydroxyethylene as transition state mimicking unit. The binding mode of this new class of compounds was predicted with automated docking and molecular dynamics simulations, with an estimation of the binding affinities through the linear interaction energy (LIE) method.
- Ersmark, Karolina,Nervall, Martin,Gutierrez-De-Teran, Hugo,Hamelink, Elizabeth,Janka, Linda K.,Clemente, Jose C.,Dunn, Ben M.,Gogoll, Adolf,Samuelsson, Bertil,Aqvist, Johan,Hallberg, Anders
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p. 2197 - 2208
(2007/10/03)
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- Macrocyclic inhibitors for peptide deformylase: A structure-activity relationship study of the ring size
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Peptide deformylase (PDF) catalyzes the removal of the N-terminal formyl group from newly synthesized polypeptides in eubacteria. Its essential role in bacterial cells but not in mammalian cells makes it an attractive target for antibacterial drug design. We have previously reported an N-formylhydroxylamine- based, metal-chelating macrocyclic PDF inhibitor, in which the P 1′ and P3′ side chains are covalently joined. In this work, we have carried out a structure-activity relationship study on the size of the macrocycle and found that 15-17-membered macrocycles are optimal for binding to the PDF active site. Unlike the acyclic compounds, which are simple competitive inhibitors, the cyclic compounds all act as slow-binding inhibitors. As compared to their acyclic counterparts, the cyclic inhibitors displayed 20-50-fold higher potency against the PDF active site (K I* as low as 70 pM), improved selectivity toward PDF, and improved the metabolic stability in rat plasma. Some of the macrocyclic inhibitors had potent, broad spectrum antibacterial activity against clinically significant Gram-positive and Gram-negative pathogens. These results suggest that the macrocyclic scaffold provides an excellent lead for the development of a new class of antibiotics.
- Hu, Xubo,Nguyen, Kiet T.,Jiang, Vernon C.,Lofland, Denene,Moser, Heinz E.,Pei, Dehua
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p. 4941 - 4949
(2007/10/03)
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- Processes for producing 7-octen-1-al and derivatives thereof
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There are disclosed a process for producing 7-octen-1-al which comprises isomerizing 2,7-octadien-1-ol in the presence of a catalyst comprising oxides of at least two metals selected from the group consisting of copper, chromium and zinc and processes for producing derivatives of 7-octen-1-al.
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