Advisor(s)

Graham B. Jones

Contributor(s)

Rein U. Kirss, George A. O'Doherty

Date of Award

2012

Date Accepted

5-2012

Degree Grantor

Northeastern University

Degree Level

M.S.

Degree Name

Master of Science

Department or Academic Unit

College of Science, Department of Chemistry & Chemical Biology

Keywords

chemistry, organic chemistry, biochemistry, biopharmaceutical, biosimilar, chemotherapeutic, PEG-ylation, radioiodination, thioether

Disciplines

Chemistry | Medicinal-Pharmaceutical Chemistry | Organic Chemistry

Abstract

Given the pressures the pharmaceutical industry is under (budgetary, regulatory, environmental, etc..), it is vital that the methods to developing safe and innovative products are continually refined. Approaches to doing so may include the development of more efficient/streamlined synthetic routes to targeted compounds, novel techniques to improve the targeting or biological properties of pharmaceuticals, innovative repurposing at the end of their patent-life, or increased use of non-invasive imaging techniques to make an early go/no-go decision. This thesis highlights three such areas of research, each an avenue towards enhancing small-molecule pharmaceuticals or better (earlier) assessment of their potential as drug candidates. Chapter 1 describes the development and optimization of advantageous transition metal catalyzed cross coupling methodology for the synthesis of aryl thioethers. Enhancement of biological properties will be examined through PEG-ylation, antibody, and ammonium salt bioconjugation in Chapter 2. Chapter 3 will explore radio-iodination methodologies for the production of SPECT imaging agents, along with a discussion of SPECT imaging and important considerations in radiosynthesis. As a conclusion, Chapter 4 will discuss the current industry shift in focus away from small-molecule to biopharmaceutical development, including a comparison between these therapies as well as considerations pertinent to biopharmaceutical design, development, manufacturing, safety, regulation, and patent protection.

Document Type

Master's Thesis

Rights Information

copyright 2012

Rights Holder

Krista Marie Wager



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