# New Methods for the Synthesis and Study of Bioactive Nitrogen-Containing Molecules

> **NIH NIH R01** · DUKE UNIVERSITY · 2020 · $260,938

## Abstract

TITLE
New Methods for the Synthesis and Study of Bioactive Nitrogen-Containing Molecules
PROJECT SUMMARY/ABSTRACT
The ubiquitous presence of nitrogen atom in small-molecule probes and drugs highlights the significance of
nitrogen-containing molecules in biomedical research and drug discovery. Rapid and efficient synthesis of
structurally diverse nitrogen-containing skeletons is of the utmost importance, as is the ability to understand
their biology, pharmacology and potential as chemical probes and drug candidates. Thus, developing new
methods for the synthesis and study of novel nitrogen-containing molecules is significant and necessary to
advance our understanding of human disease and the discovery of new therapies. The broad availability of
drugs is directly dependent on the existence of cost-efficient methods that can reliably build such novel
molecular structures and uncover their biological activity and therapeutic promise. The long-term goal of our
research is to establish a chemical platform for designing and developing novel small-molecule probes and
tools to advance the understanding and treatment of human disease. The objective of this proposal is to
develop new methods that offer rapid and efficient access to valuable nitrogen-containing building blocks for
the synthesis and study of relevant biologically active molecules and pharmaceuticals. Toward this, the
proposed strategy innovatively exploits the unique and diverse reactivity of heteroatom-nitrogen bonds––
readily available yet traditionally underutilized nitrogen precursors––to design powerful C–N bond formation
reactions that are new and different but complementary to existing methods, through the following three
specific aims: aim 1) Direct arene C–H amination and amidation via H–Zn exchange and electrophilic amino
trapping; aim 2) selective difunctionalization of alkenes by electrophilic amino activation; and aim 3) new
methods for constructing diverse azaheterocycles with facile installation of imaging tags. Successful
implementation of these studies will greatly facilitate the synthesis and study of a wide range of nitrogen-
containing molecules that are difficult or impossible to access with current technologies. With the importance of
nitrogen-containing molecules in biomedical research, new methods developed in this application and the
products generated from these transformations will have broad impact on developing novel chemical probes
and lead compounds for the understanding and treatment of disease.

## Key facts

- **NIH application ID:** 9840484
- **Project number:** 5R01GM118786-04
- **Recipient organization:** DUKE UNIVERSITY
- **Principal Investigator:** Qiu Wang
- **Activity code:** R01 (R01, R21, SBIR, etc.)
- **Funding institute:** NIH
- **Fiscal year:** 2020
- **Award amount:** $260,938
- **Award type:** 5
- **Project period:** 2017-01-05 → 2020-12-31

## Primary source

NIH RePORTER: https://reporter.nih.gov/project-details/9840484

## Citation

> US National Institutes of Health, RePORTER application 9840484, New Methods for the Synthesis and Study of Bioactive Nitrogen-Containing Molecules (5R01GM118786-04). Retrieved via AI Analytics 2026-05-22 from https://api.ai-analytics.org/grant/nih/9840484. Licensed CC0.

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