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Improved Dehydration Process for Pharmaceutical Synthesis II

Award Number: R44GM077717
ORGANIZATION: NATIONAL INSTITUTE OF GENERAL MEDICAL SCIENCES
OPDIV: NIH
AWARD CLASS: DISCRETIONARY
AWARD ACTIVITY TYPE: SCIENTIFIC/HEALTH RESEARCH (INCLUDES SURVEYS)
PERIOD OF PERFORMANCE START DATE: 09/01/2006
PERIOD OF PERFORMANCE END DATE: 08/31/2016

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Improved Dehydration Process for Pharmaceutical Synthesis II - DESCRIPTION (provided by applicant): Compact Membrane Systems (CMS) proposes to develop a perfluoro membrane reactor technology that will provide a generally applicable tool for removing water and oxygen from pharmaceutical synthesis processes. This innovation aims to improve product quality and reduce manufacturing costs of pharmaceutical end products. Manufacturing cost reductions will be derived from improved product yields, increased reaction rates and reduced energy input requirements of the manufacturing process. Product quality improvements will be derived from the elimination of entrainers, azeotropic distillation, and drying reagents in the process as well as operation at lower temperatures and driving the reactant. The project has been expanded to include the removal of both oxygen and water in an effort to reduce side reactions and/or catalyst poisoning which should be of broad use in pharmaceutical synthesis. This membrane system has the capability to withstand process temperatures of 2200C endowing it with universal applicability in almost any organic-water environment for water separation in the synthesis of products such as sildenafil, celecoxib, sertraline, and aprepitant. Given the large water-organic compound separation factors achievable, the inertness of the membrane, and the ability to withstand harsh operating conditions, we believe we have an ideal system for reaction water and oxygen removal. The proposer will develop the membrane system and processes while the subcontractors will demonstrate Pd-catalyzed amination reactions. These reactions have revolutionized drug discovery and process chemistry in the past decade. The efficiency of Pd-catalyzed amination reactions can be negatively affected by impurities such as water. The Fox group at the University of Delaware and recently hired synthesis chemists at CMS (and consultants) will demonstrate the efficacy of the membrane process in Pd-catalyzed amination reactions in a study that will consist of: synthesis of the aryl bromide intermediate from the Astra Zeneca AR-A2 process; synthesis of the Pd-catalyzed amination product from the AR-A2 process; development of GC assays for the reactions; study of a control reaction without water/oxygen removal; and, study of amination with drying of the aryl bromide intermediate using the proprietary membrane. With success in Phase I, numerous industrial partners have either already spent over $150,000 on evaluation or committed to major evaluations in Phase II.


Issue Date FY	Funding FY	Legal Entity Name	Legal Entity Address	Legal Entity City	Legal Entity State	Legal Entity Zip Code	Legal Entity COUNTY	Legal Entity COUNTRY	Assistance Listing	Award Code	Budget Year	Action Date	Action Type	Action Amount

Issue Date FY: 2017 ( Subtotal = $0 )
2017	2012	COMPACT MEMBRANE SYSTEMS, INC.	335 WATER ST	WILMINGTON	DE	19804	NEW CASTLE	USA	Biomedical Research and Research Training	000	3	1/9/2017	NON-COMPETING CONTINUATION	$0
														Subtotal = $0

Issue Date FY: 2015 ( Subtotal = $0 )
2015	2012	COMPACT MEMBRANE SYSTEMS, INC	325 HAMPTON ROAD	WILMINGTON	DE	19803	NEW CASTLE	USA	Biomedical Research and Research Training	000	3	7/6/2015	NON-COMPETING CONTINUATION	$0
														Subtotal = $0

Issue Date FY: 2014 ( Subtotal = $0 )
2014	2012	COMPACT MEMBRANE SYSTEMS, INC	325 HAMPTON ROAD	WILMINGTON	DE	19803	NEW CASTLE	USA	Biomedical Research and Research Training	000	3	7/25/2014	NON-COMPETING CONTINUATION	$0
														Subtotal = $0

Issue Date FY: 2012 ( Subtotal = $481,952 )
2012	2012	COMPACT MEMBRANE SYSTEMS, INC	335 Water St	Wilmington	DE	19804	NEW CASTLE	USA	Biomedical Research and Research Training	000	3	8/24/2012	NON-COMPETING CONTINUATION	$481,952
														Subtotal = $481,952

Issue Date FY: 2011 ( Subtotal = $546,858 )
2011	2011	COMPACT MEMBRANE SYSTEMS, INC	335 Water St	Wilmington	DE	19804	NEW CASTLE	USA	Biomedical Research and Research Training	000	2	8/22/2011	COMPETING CONTINUATION	$546,858
														Subtotal = $546,858

Grand Total All Awards = $1,028,810

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Improved Dehydration Process for Pharmaceutical Synthesis II

Award Number: R44GM077717

ORGANIZATION: NATIONAL INSTITUTE OF GENERAL MEDICAL SCIENCES

OPDIV: NIH

AWARD CLASS: DISCRETIONARY

AWARD ACTIVITY TYPE: SCIENTIFIC/HEALTH RESEARCH (INCLUDES SURVEYS)

PERIOD OF PERFORMANCE START DATE: 09/01/2006

PERIOD OF PERFORMANCE END DATE: 08/31/2016

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