# Innovative Tools for Chemical Synthesis: Metal-Hydride Catalysis, Medicinal Motifs, and Molecular Probes

> **NIH NIH R35** · UNIVERSITY OF CALIFORNIA-IRVINE · 2024 · $7,006

## Abstract

Principle Investigator/Program Director (Last, first, middle): Dong, Vy, M
Project Summary/Abstract
Asymmetric transition metal catalysis has proven time and time again to be a crucial strategy in the
pharmaceutical industry. The development of novel methods for accessing common organic scaffolds with
improvements in the areas of atom-economy and selectivity has supported the mass production of valuable drug
molecules. Hydroacylation is a powerful catalytic tool in which a hydrogen and an acyl group are added across
a site of unsaturation via transition metal catalysis. This has the potential to be useful in the construction of
carbonyl motifs for synthetic drug discovery. Azetidines are four-membered cyclic amines that can be found in
drug candidates and natural products such as Nicotianamine and Ximelagatran. Our goal, described herein, is
to explore the potential for a Rh-catalyzed asymmetric hydroacylation of azetines to generate novel azetidine
scaffolds. Switching the ligand of choice, chiral Josiphos versus 1,2-bis(diphenylphosphino)ethane dppe, allows
a regiodivergent strategy for the construction of chiral azetidines and achiral compounds. Building off of this
work, we also aim to develop further hydroacylation methods to gain access to several other strained ring
systems, which have been found to provide favorable structural and physicochemical properties necessary for
molecular optimization in modern medicinal chemistry.

## Key facts

- **NIH application ID:** 10974697
- **Project number:** 3R35GM127071-06S1
- **Recipient organization:** UNIVERSITY OF CALIFORNIA-IRVINE
- **Principal Investigator:** Vy M Dong
- **Activity code:** R35 (R01, R21, SBIR, etc.)
- **Funding institute:** NIH
- **Fiscal year:** 2024
- **Award amount:** $7,006
- **Award type:** 3
- **Project period:** 2018-05-01 → 2028-07-31

## Primary source

NIH RePORTER: https://reporter.nih.gov/project-details/10974697

## Citation

> US National Institutes of Health, RePORTER application 10974697, Innovative Tools for Chemical Synthesis: Metal-Hydride Catalysis, Medicinal Motifs, and Molecular Probes (3R35GM127071-06S1). Retrieved via AI Analytics 2026-05-22 from https://api.ai-analytics.org/grant/nih/10974697. Licensed CC0.

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