Course Catalog

Process Research in the Pharmaceutical Industry: The Design and Development of Practical Syntheses

This course on pharmaceutical process research will focus on the design and development of practical syntheses for product candidates. The importance of combining synthetic organic chemistry with physical/mechanistic organic chemistry and innovation is stressed. It is designed to expose participants to all phases of drug process development, from preclinical to New Drug Application filing. Numerous examples will be used to illustrate key aspects of process research, including issues related to US Good Manufacturing and Good Laboratory Practices (cGMP/GLP), as well as those related to the International Conference on Harmonisation of Technical Requirements for Registration of Pharmaceuticals for Human Use (ICH). Real life examples will address creativity, timeline, economic, environmental, analytical, formulation, final form, cGMP, impurity, and regulatory issues.

Course Details

Key Topics

  • Process Issues
  • Asymmetric Hydrogenations
  • Phase Transfer Chemistry

Information

This course on pharmaceutical process research will focus on the design and development of practical syntheses for product candidates. The importance of combining synthetic organic chemistry with physical/mechanistic organic chemistry and innovation is stressed. It is designed to expose participants to all phases of drug process development, from preclinical to New Drug Application filing. Numerous examples will be used to illustrate key aspects of process research, including issues related to US Good Manufacturing and Good Laboratory Practices (cGMP/GLP), as well as those related to the International Conference on Harmonisation of Technical Requirements for Registration of Pharmaceuticals for Human Use (ICH). Real life examples will address creativity, timeline, economic, environmental, analytical, formulation, final form, cGMP, impurity, and regulatory issues.

Who Should Attend

Process chemists, pharmaceutical scientists, medicinal chemists, and those involved in the development of drug manufacturing processes. Also, chemical development managers seeking additional background in the process chemistry field, or advanced undergraduate, graduate, and post-graduate students considering a career in process research. Minimally attendees should have a BS or MS in chemistry with a strong background in organic chemistry.

Agenda

  • Introduction and Overview – What is Process Research? Process research viewed through the lens of innovation.
  • Process Issues – Overview of cGMP/GLP and ICH guidelines and their application from early development to NDA filing. Selection of GMP starting materials. Management of impurity profiles during the development cycle. The interface of process chemistry and pharmaceutical formulation: API (bulk drug) and drug product?particle size distribution and surface area, purity, crystal form (polymorphs), and sterile products.
  • Modern innovative chemistry ? Handling complex molecules in chemical development of drug candidates, such as anti-methicillin-resistant staphylococcus aureus (MRSA) carbapenem and INVANZ® (ertapenem) antibiotics.
  • Crystallization – Fundamentals of crystallizations: supersaturation, nucleation, and crystal growth. Effect of crystallization processes on API properties with real life examples.
  • Asymmetric Hydrogenations ? The philosophy and role of asymmetric hydrogenations in process research with applications to the preparation of process intermediates and an anthrax lethal factor candidate.
  • Phase Transfer Chemistry ? Development of an industrial asymmetric phase transfer catalysis for the diuretic Indacrinone. Improved efficiency by a novel dual catalysis.
  • Acetylide Chemistry ? Enantioselective additions of acetylides to prochiral imines and ketones mediated by chiral aminoalkoxides ? basic research studies and application to the efavirenz (Sustiva® and Stocrin®) manufacturing process.
  • Proscar® (finasteride) development chemistry ? From medicinal chemistry to a economical manufacturing process. New dehydrogenation processes. Control of polymorphs and particle size distribution via jet mix crystallization.
  • Nucleoside Chemistry ? Development of a candidate for the treatment of hepatitis C. Special problems in chemical development of nucleoside candidates.
  • Fluoroalanine Chemistry ? The challenge of a small molecule with an apparent impossible medicinal chemistry route. Efficient deuterium use by resolution via preferential crystallization vs racemization/recycle processes.
  • Green Chemistry Strategies – Applications of diasteriomeric and asymmetric hydrogenations as well as crystallization induced diastereomeric transformations in the development of green chemical processes. JanuviaTM (sitagliptin phosphate) and Emend® (aprepitant).
  • Development examples ? Development of a practical process for the preparation of the Corey-Itsunu oxazaborolidine catalyst and applications in the preparation of ophthalmic candidates. NK-1 Receptor Antagonist and the evolution from a long linear, resolution based synthesis to a short, diastereoselective synthesis.
  • Resolutions vs Enzymes vs Asymmetric Hydrogenations – Strategies in chemical development ? the odyssey of the development of the process for cholesterol-lowering drug candidate MK-524.

Course Locations

Date

TBA

Check-in opens at 7:30 a.m. on the first day of the course.

Course runs from 8:30 a.m. to 5:00 p.m. each day.

Register Via Mail

Venue

The course fee includes a course binder and a continental breakfast each day.

Five for Four! Register five people for one course, one person for five courses, or any combination in between and your fifth registration is free. Note: This discount is only available if you register by fax or mail and mention this discount. May not be combined with any other offer.


Pricing
Early $1,395
Advanced $1,495
Standard $1,595

About the Instructors

  • Dr. Ed Grabowski

    (B.S. MIT, Ph. D. Univ. of Rochester) was Vice President of Chemistry in Process Research at his retirement and teaches Process Research in the Pharmaceutical Industry: The Design and Development of Practical Syntheses.

  • Dr. Ulf Dolling

    (B.S. Univ. of Hamburg, Ph.D. Rutgers) was Executive Director of Process Research prior to his retirement in 2005 and teaches Process Research in the Pharmaceutical Industry: The Design and Development of Practical Syntheses.