Automated and Accelerated Synthesis of Indole Derivatives on a Nano-Scale.

ABSTRACT: Automated, miniaturized and accelerated synthesis for efficient property optimization is a formidable challenge for chemistry in the 21st century as it helps to reduce resources and waste and can deliver products in shorter time frames. Here, we used for the first-time acoustic droplet ejection (ADE) technology and fast quality control to screen efficiency of synthetic reactions on a nanomole scale in an automated and miniaturized fashion. The interrupted Fischer indole combined with Ugi-type reactions yielded several attractive drug-like scaffolds. In 384-well plates, a diverse set of interrupted Fischer indole intermediates were produced and reacted to the tricyclic hydantoin backbone by a 2-step sequence. Similarly, preformed Fischer indole intermediates were used to produce divers sets

SUBMITTER: Shaabani S 

PROVIDER: S-EPMC6342289 | biostudies-literature | 2019 Jan

REPOSITORIES: biostudies-literature