Development of an efficient route toward meiogynin A-inspired dual inhibitors of Bcl-xL and Mcl-1 anti-apoptotic proteins

2015 ◽  
Vol 13 (19) ◽  
pp. 5520-5531 ◽  
Author(s):  
Sandy Desrat ◽  
Camille Remeur ◽  
Fanny Roussi
Keyword(s):  
Good Yield ◽  
Large Scale ◽  
Efficient Strategy ◽  
Efficient Route ◽  
Dual Inhibitors ◽  
Apoptotic Proteins

The synthesis, on a large scale, with very good yield and er via an efficient strategy, of a chiral 4-substituted 2-cyclohexenone intermediate, was a milestone in the synthesis of seven analogues of meiogynin A, a natural sesquiterpenoid dimer.

scholarly journals An efficient strategy for large scale 3D simulation of heterogeneous materials to predict effective thermal conductivity

2019 ◽  
Vol 166 ◽  
pp. 265-275 ◽  
Author(s):  
Xiaodong Liu ◽  
Julien Réthoré ◽  
Marie-Christine Baietto ◽  
Philippe Sainsot ◽  
Antonius Adrianus Lubrecht
Keyword(s):  
Thermal Conductivity ◽  
Effective Thermal Conductivity ◽  
Large Scale ◽  
Heterogeneous Materials ◽  
3D Simulation ◽  
Efficient Strategy

A simple and efficient strategy for solving very large-scale generalized cable-trench problems

Networks ◽  
2015 ◽  
Vol 67 (3) ◽  
pp. 199-208 ◽  
Author(s):  
Francis J. Vasko ◽  
Eric Landquist ◽  
Gregory Kresge ◽  
Adam Tal ◽  
Yifeng Jiang ◽  
...  
Keyword(s):  
Large Scale ◽  
Efficient Strategy

Synthesis of novel carbohydrate mimetics via 1,2-oxazines

2011 ◽  
Vol 84 (1) ◽  
pp. 23-36 ◽  
Author(s):  
Léa Bouché ◽  
Hans-Ulrich Reissig
Keyword(s):  
Lewis Acid ◽  
Good Yield ◽  
Biological Activities ◽  
Amino Sugar ◽  
Sugar Alcohols ◽  
Bicyclic Compounds ◽  
Efficient Route ◽  
Oxazine Derivatives

The combination of lithiated alkoxyallenes with carbohydrate-derived nitrones constitutes a flexible entry to highly functionalized enantiopure 1,2-oxazine derivatives. They can be used as precursors for acyclic and cyclic carbohydrate-like products such as amino sugar alcohols, azetidine and pyrrolidine derivatives. The Lewis acid-promoted rearrangement of 1,3-dioxolanyl-substituted 1,2-oxazines to bicyclic compounds allows an efficient route to novel amino pyran and oxepane derivatives. After subsequent transformations, new carbohydrate mimetics or “real” carbohydrates were obtained in good yield and often in a stereodivergent fashion. These compounds have already been employed for the preparation of unusual di- and trisaccharide derivatives. Several of the products prepared showed interesting biological activities, e.g., as L- and P-selectin inhibitors with IC50 values in the subnanomolar range.

Orthogonally Protected Monosaccharide Building Blocks for Solid Phase Production of Diversity Oriented Libraries

2010 ◽  
Vol 63 (4) ◽  
pp. 693 ◽  
Author(s):  
Premraj Rajaratnam ◽  
Praveer Gupta ◽  
Peter Katavic ◽  
Krystle Kuipers ◽  
Ngoc Huyh ◽  
...  
Keyword(s):  
Good Yield ◽  
Large Scale ◽  
Solid Phase ◽  
Building Blocks ◽  
Chromatographic Purification ◽  
Large Scale Synthesis ◽  
Phase Production

The large scale synthesis of three orthogonally protected monosaccharide scaffolds suitable for use in the solid phase preparation of large diversity libraries is presented. Scaffolds based on 2-amino-2-deoxy-d-glucopyranose, 2-amino-2-deoxy-d-allopyranose, and 2,4-diamino-2,4-dideoxy-d-galactopyranose were prepared in good yield and with minimal chromatographic purification from commercially available methyl 2-azido-2-deoxy-1-thio-β-d-glucopyranose and methyl 2-amino-2-deoxy-1-thio-β-d-glucopyranose.

An efficient strategy for the large-scale synthesis of head-to-tail cyclic peptides

1994 ◽  
Vol 1 (1) ◽  
pp. 25-30 ◽  
Author(s):  
John X. He ◽  
Wayne L. Cody ◽  
Annette M. Doherty
Keyword(s):  
Cyclic Peptides ◽  
Large Scale ◽  
Efficient Strategy ◽  
Large Scale Synthesis

scholarly journals Multi-Gram Synthesis of Enantiopure 1,5-Disubstituted Tetrazoles Via Ugi-Azide 3-Component Reaction

Molecules ◽  
2018 ◽  
Vol 23 (11) ◽  
pp. 2758 ◽  
Author(s):  
Pietro Capurro ◽  
Lisa Moni ◽  
Andrea Galatini ◽  
Christian Mang ◽  
Andrea Basso
Keyword(s):  
Large Scale ◽  
Combinatorial Libraries ◽  
Biological Properties ◽  
Target Product ◽  
Three Component Reaction ◽  
Efficient Route ◽  
Large Scale Synthesis

Tetrazoles have been widely studied for their biological properties. An efficient route for large-scale synthesis of 1,5-disubstituted tetrazoles (1,5-DTs) is presented. The strategy exploits a reductive approach to synthetize a cyclic chiral imine substrate which is then converted into the target product through an Ugi-azide three-component reaction (UA-3CR). The final products are equipped with additional functionalities which can be further elaborated for the generation of combinatorial libraries of enantiopure heterocycles.

scholarly journals Development of dynamic kinetic resolution on large scale for (±)-1-phenylethylamine

2010 ◽  
Vol 6 ◽  
pp. 823-829 ◽  
Author(s):  
Lisa K Thalén ◽  
Jan-E Bäckvall
Keyword(s):  
Good Yield ◽  
Large Scale ◽  
Kinetic Resolution ◽  
Catalyst Loading ◽  
Acyl Donor ◽  
Dynamic Kinetic Resolution ◽  
Reaction Parameters ◽  
Ru Catalyst ◽  
Isopropyl Acetate ◽  
Acyl Donors

Candida antarctica lipase B (CALB) and racemization catalyst 4 were combined in the dynamic kinetic resolution (DKR) of (±)-1-phenylethylamine (1). Several reaction parameters have been investigated to modify the method for application on multigram scale. A comparison of isopropyl acetate and alkyl methoxyacetates as acyl donors was carried out. It was found that lower catalyst loadings could be used to obtain (R)-2-methoxy-N-(1-phenylethyl)acetamide (3) in good yield and high ee when alkyl methoxyacetates were used as acyl donors compared to when isopropyl acetate was used as the acyl donor. The catalyst loading could be decreased to 1.25 mol % Ru-catalyst 4 and 10 mg CALB per mmol 1 when alkyl methoxyacetates were used as the acyl donor.

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