# Chemical Synthesis

> **NIH NIH P30** · ALBERT EINSTEIN COLLEGE OF MEDICINE · 2020 · $81,843

## Abstract

PROJECT SUMMARY – CHEMICAL SYNTHESIS SHARED RESOURCE
The Chemical Synthesis Shared Resource, in development for several years, is proposed in this application
as an established AECC shared resource. The objective of this facility is to design and synthesize novel small
organic molecules in support of AECC research. The facility is staffed by a group of experienced chemists that
have established a track-record of providing drugs and reagents in support of AECC research projects. These
include novel first-in-class agents that are in the process of translation into novel cancer therapeutics. The
facility provides: (i) Consultation in design/synthesis/compound verification. Investigators provide an overview
of the target and the biological pathway following which staff research possible chemotypes previously
reported by in silico or experimental screening. (ii) A synthetic route to the desired compound is designed
along with alternative strategies. (iii) A small-scale (20-50 mg) “proof-of-principle” synthesis is completed and
validated chemically following which the biological or pharmacological effect is confirmed. (iv) The synthesis is
then scaled-up and the large scale batch synthesis validated by analytical HPLC, UV-visible
spectrophotometry, mass spectrometry and multinuclear (1H, 13C) NMR. Chemical stability (pH and
temperature) and aqueous solubility or solubility in mixed solvents can be documented. The facility can assist
investigators with more detailed SAR, when necessary, to further improve the properties of molecules once a
synthesized compound has been shown to have the desired action. The additional chemical “space” around
the original compound can be probed and, since synthetic precursors to the original compound are often
retained, substituent variations can made relatively quickly. In this way, an originally identified compound with
activity can be “built out” with resulting increases in potency. There are a number of examples in which this has
been achieved. In other cases, a known chemotype has been modified to enhance stability and cell
permeability. The facility has also purchased or synthesized a large number of alkynes and aliphatic and
aromatic azides. When paired these “click” reactants will react, catalyzed by Cu(I) by a cycloaddition to
generate a triazole ring with excellent chemical and biological stability. The Facility has generated three novel
chelators that enhance the reactivity of the copper catalyst and also reduce the inherent toxicity of copper in
biological systems, allowing for these reactions to be performed on cells and tissues. These chelators are
available to AECC investigators and frequently provided to the broader scientific community at modest cost.
The facility provides AECC investigators with publication-quality details of the synthesis and analytical
validation.

## Key facts

- **NIH application ID:** 9998875
- **Project number:** 5P30CA013330-48
- **Recipient organization:** ALBERT EINSTEIN COLLEGE OF MEDICINE
- **Principal Investigator:** John S Blanchard
- **Activity code:** P30 (R01, R21, SBIR, etc.)
- **Funding institute:** NIH
- **Fiscal year:** 2020
- **Award amount:** $81,843
- **Award type:** 5
- **Project period:** 1997-06-01 → 2022-06-30

## Primary source

NIH RePORTER: https://reporter.nih.gov/project-details/9998875

## Citation

> US National Institutes of Health, RePORTER application 9998875, Chemical Synthesis (5P30CA013330-48). Retrieved via AI Analytics 2026-05-22 from https://api.ai-analytics.org/grant/nih/9998875. Licensed CC0.

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