scholarly journals Traceless Staudinger ligation enabled parallel synthesis of proteolysis targeting chimera linker variants

2021 ◽  
Author(s):  
Troy A. Bemis ◽  
James J. La Clair ◽  
Michael D. Burkart
Keyword(s):  
Small Molecule ◽  
Parallel Synthesis ◽  
Staudinger Ligation ◽  
One Pot

Chemoselectivity of the traceless Staudinger ligation was leveraged to enable assembly of chimeric small-molecule linker variants in a one-pot approach.

scholarly journals Synthesis of pentasubstituted 2-aryl pyrroles from boryl and stannyl alkynes via one-pot sequential Ti-catalyzed [2 + 2 + 1] pyrrole synthesis/cross coupling reactions

2020 ◽  
Vol 11 (37) ◽  
pp. 10236-10242
Author(s):  
Yukun Cheng ◽  
Channing K. Klein ◽  
Ian A. Tonks
Keyword(s):  
Small Molecule ◽  
Cross Coupling ◽  
Coupling Reactions ◽  
One Pot ◽  
Cross Coupling Reactions

Multisubstituted pyrroles are commonly found in many bioactive small molecule scaffolds, yet the synthesis of highly-substituted pyrrole cores remains challenging.

scholarly journals Identification of Bis-Cyclic Guanidines as Antiplasmodial Compounds from Positional Scanning Mixture-Based Libraries

Molecules ◽  
2019 ◽  
Vol 24 (6) ◽  
pp. 1100 ◽  
Author(s):  
David Perry ◽  
Bracken Roberts ◽  
Ginamarie Debevec ◽  
Heather Michaels ◽  
Debopam Chakrabarti ◽  
...  
Keyword(s):  
Small Molecule ◽  
Parallel Synthesis ◽  
Variable Position ◽  
Positional Scanning ◽  
Small Molecule Libraries ◽  
The Individual

The screening of more than 30 million compounds derived from 81 small molecule libraries built on 81 distinct scaffolds identified pyrrolidine bis-cyclic guanidine library (TPI-1955) to be one of the most active and selective antiplasmodial libraries. The screening of the positional scanning library TPI-1955 arranged on four sets of sublibraries (26 + 26 + 26 + 40), totaling 120 samples for testing provided information about the most important groups of each variable position in the TPI-1955 library containing 738,192 unique compounds. The parallel synthesis of the individual compounds derived from the deconvolution of the positional scanning library led to the identification of active selective antiplasmodial pyrrolidine bis-cyclic guanidines.

Parallel Synthesis of Antimalarial Rhodacyanine Dyes by the Combination of Three Components in One Pot

2003 ◽  
Vol 5 (3) ◽  
pp. 211-214 ◽  
Author(s):  
Kiyosei Takasu ◽  
Hiroki Terauchi ◽  
Hiroshi Inoue ◽  
Hye-Sook Kim ◽  
Yusuke Wataya ◽  
...  
Keyword(s):  
Parallel Synthesis ◽  
One Pot ◽  
Three Components

scholarly journals “Exhaustive” Baeyer-Villiger Oxidation of Poly(Methyl Vinyl Ketone) and Its Copolymers

2021 ◽  
Author(s):  
Pengfei Ma ◽  
Christopher M. Plummer ◽  
Luo Wenjun ◽  
Jiyan Pang ◽  
Yongming Chen ◽  
...  
Keyword(s):  
Block Copolymers ◽  
Small Molecule ◽  
Chain Scission ◽  
Side Reactions ◽  
One Pot ◽  
Methyl Vinyl ◽  
Modification Procedure ◽  
Post Modification ◽  
User Friendly ◽  
Villiger Oxidation

The development of “exhaustive” (nearly quantitative) post-modification reactions relies heavily on the efficiency of their corresponding small-molecule protocols. However, the direct translation of existing small-molecule protocols into post-polymerization modifications were often troublesome due to undesired side reactions. For example, the development of an “exhaustive” BaeyerVilliger (BV) post-modification using existing small-molecule BV protocols suffered from a lack of reactivity or significant chain scission. Herein, we demonstrate that a careful re-optimization of a small-molecule transformation on a polymer substrate allowed us to overcome such challenges, thereby enabling an “exhaustive” BV post-polymerization modification. Furthermore, a one-pot copolymerization/“exhaustive” BV post-modification procedure was developed to produce copolymers of vinyl acetate (VAc) and more activated monomers (MAMs) in a convenient and scalable manner. This user-friendly methodology provides a general access to synthetically challenging poly(VAc-co-MAM)s including both statistical and narrow-dispersed block copolymers and could greatly facilitate the exploration of applications with such materials.

scholarly journals Synthesis of Elaborate Benzofuran-2-Carboxamide Derivatives through a Combination of 8-Aminoquinoline Directed C–H Arylation and Transamidation Chemistry

Molecules ◽  
2020 ◽  
Vol 25 (2) ◽  
pp. 361
Author(s):  
Michael Oschmann ◽  
Linus Johansson Holm ◽  
Monireh Pourghasemi-Lati ◽  
Oscar Verho
Keyword(s):  
Small Molecule ◽  
High Efficiency ◽  
Synthetic Route ◽  
One Pot ◽  
Synthetic Strategy ◽  
Small Molecule Screening ◽  
Wide Range ◽  
Directing Group

Herein, we present a short and highly modular synthetic route that involves 8-aminoquinoline directed C–H arylation and transamidation chemistry, and which enables access to a wide range of elaborate benzofuran-2-carboxamides. For the directed C–H arylation reactions, Pd catalysis was used to install a wide range of aryl and heteroaryl substituents at the C3 position of the benzofuran scaffold in high efficiency. Directing group cleavage and further diversification of the C3-arylated benzofuran products were then achieved in a single synthetic operation through the utilization of a one-pot, two-step transamidation procedure, which proceeded via the intermediate N-acyl-Boc-carbamates. Given the high efficiency and modularity of this synthetic strategy, it constitutes a very attractive method for generating structurally diverse collections of benzofuran derivatives for small molecule screening campaigns.

Staudinger Ligation: A New Immobilization Strategy for the Preparation of Small-Molecule Arrays

2003 ◽  
Vol 42 (47) ◽  
pp. 5830-5834 ◽  
Author(s):  
Maja Köhn ◽  
Ron Wacker ◽  
Carsten Peters ◽  
Hendrik Schröder ◽  
Laurent Soulère ◽  
...  
Keyword(s):  
Small Molecule ◽  
Staudinger Ligation

Solvent-free accelerated organic syntheses using microwaves

2001 ◽  
Vol 73 (1) ◽  
pp. 193-198 ◽  
Author(s):  
Rajender S. Varma
Keyword(s):  
Organic Synthesis ◽  
High Speed ◽  
Multicomponent Reactions ◽  
Solvent Free ◽  
Parallel Synthesis ◽  
One Pot ◽  
Reduction Reactions ◽  
Heterocyclic Molecules ◽  
Organic Syntheses

A solvent-free approach for organic synthesis is described which involves microwave (MW) exposure of neat reactants (undiluted) either in the presence of a catalyst or catalyzed by the surfaces of inexpensive and recyclable mineral supports such as alumina, silica, clay, or "doped" surfaces, namely, Fe(NO3)3-clay (clayfen), Cu(NO3)2-clay (claycop), NH2OH-clay, PhI(OAc)2-alumina, NaIO4-silica, MnO2-silica, and NaBH4-clay. A variety of deprotection, condensation, cyclization, oxidation, and reduction reactions are presented including the efficient one-pot assembly of heterocyclic molecules from in situ generated intermediates such as enamines and a-tosyloxyketones. The application of this solvent-free MW approach to multicomponent reactions is highlighted that can be adapted for high-speed parallel synthesis of the library of dihydropyrimidine-2(1H)-ones and imidazo [1,2-a]annulated pyridines, pyrazines, and pyrimidines.

scholarly journals 2,2,2-Trifluoroethyl Oxalates in the One-Pot Parallel Synthesis of Hindered Aliphatic Oxamides (Eur. J. Org. Chem. 12/2016)

2016 ◽  
Vol 2016 (12) ◽  
Author(s):  
Andrey V. Bogolubsky ◽  
Yurii S. Moroz ◽  
Pavel K. Mykhailiuk ◽  
Sergey E. Pipko ◽  
Alexander V. Grishchenko ◽  
...  
Keyword(s):  
Parallel Synthesis ◽  
One Pot ◽  
The One
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