The Nonchiral Bislactim Diethoxy Ether as a Highly Stereo-Inducing Synthon for Sterically Hindered,γ-Branchedα-Amino Acids: A Practical, Large-Scale Route to an Intermediate of the Novel Renin Inhibitor Aliskiren

2003 ◽  
Vol 86 (8) ◽  
pp. 2848-2870 ◽  
Author(s):  
Richard Göschke ◽  
Stefan Stutz ◽  
Walter Heinzelmann ◽  
Jürgen Maibaum
2019 ◽  
Author(s):  
Yongzheng Ding ◽  
Shuai Fan ◽  
Xiaoxi Chen ◽  
yuzhen gao ◽  
Gang Li

A Pdᴵᴵ-catalyzed, ligand-enabled gamma-C(sp3)–H arylation of free primary aliphatic amines and amino esters without using an exogenous directing group is reported. This reaction is compatible with unhindered free aliphatic amines, and it is also be applicable to the rapid synthesis of biologically and synthetically valuable unnatural α-amino acids. Large scale synthesis is also feasible using this method.<br>


2019 ◽  
Author(s):  
Mingguang Chen ◽  
Wangxiang Li ◽  
Anshuman Kumar ◽  
Guanghui Li ◽  
Mikhail Itkis ◽  
...  

<p>Interconnecting the surfaces of nanomaterials without compromising their outstanding mechanical, thermal, and electronic properties is critical in the design of advanced bulk structures that still preserve the novel properties of their nanoscale constituents. As such, bridging the p-conjugated carbon surfaces of single-walled carbon nanotubes (SWNTs) has special implications in next-generation electronics. This study presents a rational path towards improvement of the electrical transport in aligned semiconducting SWNT films by deposition of metal atoms. The formation of conducting Cr-mediated pathways between the parallel SWNTs increases the transverse (intertube) conductance, while having negligible effect on the parallel (intratube) transport. In contrast, doping with Li has a predominant effect on the intratube electrical transport of aligned SWNT films. Large-scale first-principles calculations of electrical transport on aligned SWNTs show good agreement with the experimental electrical measurements and provide insight into the changes that different metal atoms exert on the density of states near the Fermi level of the SWNTs and the formation of transport channels. </p>


2008 ◽  
Vol 59 (11) ◽  
Author(s):  
Iulia Lupan ◽  
Sergiu Chira ◽  
Maria Chiriac ◽  
Nicolae Palibroda ◽  
Octavian Popescu

Amino acids are obtained by bacterial fermentation, extraction from natural protein or enzymatic synthesis from specific substrates. With the introduction of recombinant DNA technology, it has become possible to apply more rational approaches to enzymatic synthesis of amino acids. Aspartase (L-aspartate ammonia-lyase) catalyzes the reversible deamination of L-aspartic acid to yield fumaric acid and ammonia. It is one of the most important industrial enzymes used to produce L-aspartic acid on a large scale. Here we described a novel method for [15N] L-aspartic synthesis from fumarate and ammonia (15NH4Cl) using a recombinant aspartase.


IoT ◽  
2021 ◽  
Vol 2 (1) ◽  
pp. 140-162
Author(s):  
Hung Nguyen-An ◽  
Thomas Silverston ◽  
Taku Yamazaki ◽  
Takumi Miyoshi

We now use the Internet of things (IoT) in our everyday lives. The novel IoT devices collect cyber–physical data and provide information on the environment. Hence, IoT traffic will count for a major part of Internet traffic; however, its impact on the network is still widely unknown. IoT devices are prone to cyberattacks because of constrained resources or misconfigurations. It is essential to characterize IoT traffic and identify each device to monitor the IoT network and discriminate among legitimate and anomalous IoT traffic. In this study, we deployed a smart-home testbed comprising several IoT devices to study IoT traffic. We performed extensive measurement experiments using a novel IoT traffic generator tool called IoTTGen. This tool can generate traffic from multiple devices, emulating large-scale scenarios with different devices under different network conditions. We analyzed the IoT traffic properties by computing the entropy value of traffic parameters and visually observing the traffic on behavior shape graphs. We propose a new method for identifying traffic entropy-based devices, computing the entropy values of traffic features. The method relies on machine learning to classify the traffic. The proposed method succeeded in identifying devices with a performance accuracy up to 94% and is robust with unpredictable network behavior with traffic anomalies spreading in the network.


Healthcare ◽  
2021 ◽  
Vol 9 (2) ◽  
pp. 126
Author(s):  
Hai-Feng Ling ◽  
Zheng-Lian Su ◽  
Xun-Lin Jiang ◽  
Yu-Jun Zheng

In a large-scale epidemic, such as the novel coronavirus pneumonia (COVID-19), there is huge demand for a variety of medical supplies, such as medical masks, ventilators, and sickbeds. Resources from civilian medical services are often not sufficient for fully satisfying all of these demands. Resources from military medical services, which are normally reserved for military use, can be an effective supplement to these demands. In this paper, we formulate a problem of integrated civilian-military scheduling of medical supplies for epidemic prevention and control, the aim of which is to simultaneously maximize the overall satisfaction rate of the medical supplies and minimize the total scheduling cost, while keeping a minimum ratio of medical supplies reservation for military use. We propose a multi-objective water wave optimization (WWO) algorithm in order to efficiently solve this problem. Computational results on a set of problem instances constructed based on real COVID-19 data demonstrate the effectiveness of the proposed method.


Author(s):  
Anna Lavecchia ◽  
Matteo Chiara ◽  
Caterina De Virgilio ◽  
Caterina Manzari ◽  
Carlo Pazzani ◽  
...  

Abstract Staphylococcus cohnii (SC), a coagulase-negative bacterium, was first isolated in 1975 from human skin. Early phenotypic analyses led to the delineation of two subspecies (subsp.), Staphylococcus cohnii subsp. cohnii (SCC) and Staphylococcus cohnii subsp. urealyticus (SCU). SCC was considered to be specific to humans whereas SCU apparently demonstrated a wider host range, from lower primates to humans. The type strains ATCC 29974 and ATCC 49330 have been designated for SCC and SCU, respectively. Comparative analysis of 66 complete genome sequences—including a novel SC isolate—revealed unexpected patterns within the SC complex, both in terms of genomic sequence identity and gene content, highlighting the presence of 3 phylogenetically distinct groups. Based on our observations, and on the current guidelines for taxonomic classification for bacterial species, we propose a revision of the SC species complex. We suggest that SCC and SCU should be regarded as two distinct species: SC and SU (Staphylococcus urealyticus), and that two distinct subspecies, SCC and SCB (SC subsp. barensis, represented by the novel strain isolated in Bari) should be recognized within SC. Furthermore, since large scale comparative genomics studies recurrently suggest inconsistencies or conflicts in taxonomic assignments of bacterial species, we believe that the approach proposed here might be considered for more general application.


2021 ◽  
Vol 40 (5) ◽  
pp. 10043-10061
Author(s):  
Xiaoping Shi ◽  
Shiqi Zou ◽  
Shenmin Song ◽  
Rui Guo

 The asset-based weapon target assignment (ABWTA) problem is one of the important branches of the weapon target assignment (WTA) problem. Due to the current large-scale battlefield environment, the ABWTA problem is a multi-objective optimization problem (MOP) with strong constraints, large-scale and sparse properties. The novel model of the ABWTA problem with the operation error parameter is established. An evolutionary algorithm for large-scale sparse problems (SparseEA) is introduced as the main framework for solving large-scale sparse ABWTA problem. The proposed framework (SparseEA-ABWTA) mainly addresses the issue that problem-specific initialization method and genetic operators with a reward strategy can generate solutions efficiently considering the sparsity of variables and an improved non-dominated solution selection method is presented to handle the constraints. Under the premise of constructing large-scale cases by the specific case generator, two numerical experiments on four outstanding multi-objective evolutionary algorithms (MOEAs) show Runtime of SparseEA-ABWTA is faster nearly 50% than others under the same convergence and the gap between MOEAs improved by the mechanism of SparseEA-ABWTA and SparseEA-ABWTA is reduced to nearly 20% in the convergence and distribution.


2021 ◽  
Vol 9 (6) ◽  
pp. 1110
Author(s):  
Ángel Córcoles García ◽  
Peter Hauptmann ◽  
Peter Neubauer

Insufficient mixing in large-scale bioreactors provokes gradient zones of substrate, dissolved oxygen (DO), pH, and other parameters. E. coli responds to a high glucose, low oxygen feeding zone with the accumulation of mixed acid fermentation products, especially formate, but also with the synthesis of non-canonical amino acids, such as norvaline, norleucine and β-methylnorleucine. These amino acids can be mis-incorporated into recombinant products, which causes a problem for pharmaceutical production whose solution is not trivial. While these effects can also be observed in scale down bioreactor systems, these are challenging to operate. Especially the high-throughput screening of clone libraries is not easy, as fed-batch cultivations would need to be controlled via repeated glucose pulses with simultaneous oxygen limitation, as has been demonstrated in well controlled robotic systems. Here we show that not only glucose pulses in combination with oxygen limitation can provoke the synthesis of these non-canonical branched-chain amino acids (ncBCAA), but also that pyruvate pulses produce the same effect. Therefore, we combined the enzyme-based glucose delivery method Enbase® in a PALL24 mini-bioreactor system and combined repeated pyruvate pulses with simultaneous reduction of the aeration rate. These cultivation conditions produced an increase in the non-canonical branched chain amino acids norvaline and norleucine in both the intracellular soluble protein and inclusion body fractions with mini-proinsulin as an example product, and this effect was verified in a 15 L stirred tank bioreactor (STR). To our opinion this cultivation strategy is easy to apply for the screening of strain libraries under standard laboratory conditions if no complex robotic and well controlled parallel cultivation devices are available.


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