# Stereospecific cross-coupling reactions as a tool for three-dimensional molecular diversification

> **NIH NIH R01** · CITY COLLEGE OF NEW YORK · 2020 · $307,160

## Abstract

PROJECT SUMMARY/ABSTRACT
Using enantioenriched organometallic nucleophiles in palladium-catalyzed carbon-carbon bond-
forming reactions, we aim to develop general tools for the rapid preparation of non-racemic
biologically active molecules. By establishing the final stereogenic configuration prior to the
formation of the final desired bond, the rapid preparation of diverse libraries of single-
enantiomer drug candidates for use in biological assays will be achievable. The use of optically
active secondary alkylboron and alkylstannane nucleophiles will initially be explored in Pd-
catalyzed alkyl-aryl cross-coupling reactions, with particular focus on the derivatization of
medicinally relevant organic frameworks. The inclusion of heterocycles will be emphasized in
order to maximize access to chiral structural motifs that are currently inaccessible but are of
biological or pharmaceutical interest.

## Key facts

- **NIH application ID:** 9975863
- **Project number:** 5R01GM131079-03
- **Recipient organization:** CITY COLLEGE OF NEW YORK
- **Principal Investigator:** Mark Roger Biscoe
- **Activity code:** R01 (R01, R21, SBIR, etc.)
- **Funding institute:** NIH
- **Fiscal year:** 2020
- **Award amount:** $307,160
- **Award type:** 5
- **Project period:** 2018-09-15 → 2022-05-31

## Primary source

NIH RePORTER: https://reporter.nih.gov/project-details/9975863

## Citation

> US National Institutes of Health, RePORTER application 9975863, Stereospecific cross-coupling reactions as a tool for three-dimensional molecular diversification (5R01GM131079-03). Retrieved via AI Analytics 2026-05-23 from https://api.ai-analytics.org/grant/nih/9975863. Licensed CC0.

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