Artigo Acesso aberto Revisado por pares

Nanomole-scale high-throughput chemistry for the synthesis of complex molecules

2014; American Association for the Advancement of Science; Volume: 347; Issue: 6217 Linguagem: Inglês

10.1126/science.1259203

ISSN

1095-9203

Autores

A. Buitrago Santanilla, Erik L. Regalado, Tony Pereira, Michael Shevlin, Kevin P. Bateman, Louis‐Charles Campeau, Jonathan E. Schneeweis, Simon Berritt, Zhicai Shi, Philippe G. Nantermet, Yong Liu, Roy Helmy, Christopher J. Welch, Petr Váchal, Ian W. Davies, Tim Cernak, Spencer D. Dreher,

Tópico(s)

Computational Drug Discovery Methods

Resumo

Breaking through the milligram floor When chemists synthesize compounds, the threshold for success is at least a milligram of product. This has been true for decades—even though biochemical assays have long since descended into microgram territory—and results in part from the constraints of characterization methods. Buitrago Santanilla et al. present an automated dosing and characterization protocol for optimizing chemical reaction conditions on the microgram scale. This allowed them to screen numerous base and ligand combinations for catalytic C-N bond-forming reactions between complex pairs of compounds, in short supply, that resisted standard coupling conditions. Science , this issue p. 49

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