# Selective Functionalization of Aliphatic Amines and Derivatives

> **NIH NIH R01** · COLUMBIA UNIV NEW YORK MORNINGSIDE · 2020 · $268,598

## Abstract

Project Summary
Modern drug discovery mandates the rapid and modular assembly of increasingly complex substances.
Medicinally relevant molecules overwhelmingly bear nitrogen functionality with 910 of 1086 FDA small
molecule drugs contain at least one N-atom. Of the Top 200 drugs by retail sales (2012), 73% are small-
molecule based. Of these, 67% bear an aliphatic amine defined as having nitrogen not part of a heterocycle or
aniline system. Functionalizing simple amine based precursors directly at C-H bonds is a significant problem.
This proposal describes several strategies aimed at addressing this problem relying o complementary
strategies to achieve the goal. The resultant products will facilitate the pace of drug discovery, with the
common motifs visible in biologically active agents ranging from antibiotics, antidepressants among many
others. The specific goals of this research are as follows:
1) Develop a unified protocol for δ functionalization of amines by 1,5 hydrogen atom transfer;
2) Exploit different directing groups on nitrogen to achieve complementary site selectivity;
3) Expand radical couples by merging cobalt and photoredox catalysis.
The long-term impact of this science is to enable chemists to rapidly assemble complex structures with high
efficiency.

## Key facts

- **NIH application ID:** 9901587
- **Project number:** 5R01GM125206-04
- **Recipient organization:** COLUMBIA UNIV NEW YORK MORNINGSIDE
- **Principal Investigator:** Tomislav Rovis
- **Activity code:** R01 (R01, R21, SBIR, etc.)
- **Funding institute:** NIH
- **Fiscal year:** 2020
- **Award amount:** $268,598
- **Award type:** 5
- **Project period:** 2017-07-01 → 2021-06-30

## Primary source

NIH RePORTER: https://reporter.nih.gov/project-details/9901587

## Citation

> US National Institutes of Health, RePORTER application 9901587, Selective Functionalization of Aliphatic Amines and Derivatives (5R01GM125206-04). Retrieved via AI Analytics 2026-05-23 from https://api.ai-analytics.org/grant/nih/9901587. Licensed CC0.

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