‘Chemistry at the speed of sound’: automated 1536-well nanoscale synthesis of 16 scaffolds in parallel

Result code in IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F61989592%3A15640%2F23%3A73621359" target="_blank" >RIV/61989592:15640/23:73621359 - isvavai.cz</a>

Result on the web

<a href="https://pubs.rsc.org/en/content/articlelanding/2023/GC/D2GC04312B" target="_blank" >https://pubs.rsc.org/en/content/articlelanding/2023/GC/D2GC04312B</a>

DOI - Digital Object Identifier

<a href="http://dx.doi.org/10.1039/d2gc04312b" target="_blank" >10.1039/d2gc04312b</a>

Result language

angličtina

Original language name

‘Chemistry at the speed of sound’: automated 1536-well nanoscale synthesis of 16 scaffolds in parallel

Original language description

Screening of large and diverse libraries is the &apos;bread and butter&apos; in the first phase of the discovery of novel drugs. However, maintenance and periodic renewal of high-quality large compound collections pose considerable logistic, environmental and monetary problems. Here, we exercise an alternative, the &apos;on-the-fly&apos; synthesis of large and diverse libraries on a nanoscale in a highly automated fashion. For the first time, we show the feasibility of the synthesis of a large library based on 16 different chemistries in parallel on several 384-well plates using the acoustic dispensing ejection (ADE) technology platform. In contrast to combinatorial chemistry, we produced 16 scaffolds at the same time and in a sparse matrix fashion, and each compound was produced by a random combination of diverse large building blocks. The synthesis, analytics, resynthesis of selected compounds, and chemoinformatic analysis of the library are described. The advantages of the herein described automated nanoscale synthesis approach include great library diversity, absence of library storage logistics, superior economics, speed of synthesis by automation, increased safety, and hence sustainable chemistry.

Czech name

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Czech description

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Type

J_imp - Article in a specialist periodical, which is included in the Web of Science database

CEP classification

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OECD FORD branch

10401 - Organic chemistry

Project

—

Continuities

I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace

Publication year

2023

Confidentiality

S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Name of the periodical

GREEN CHEMISTRY

ISSN

1463-9262

e-ISSN

1463-9270

Volume of the periodical

25

Issue of the periodical within the volume

4

Country of publishing house

GB - UNITED KINGDOM

Number of pages

15

Pages from-to

"1380 "- 1394

UT code for WoS article

000919843800001

EID of the result in the Scopus database

2-s2.0-85147153280