National Cancer Institute, Research Contracts Branch, PSAS, 6120 Executive Blvd, EPS/Room 638, Bethesda, MD 20892-7227

68 -- SYNTHESIS OF PHOSPHORAMIDITES OF CONFORMATIONALLY LOCKED CARBOCYCLIC NUCLEOSIDES TO ELUCIDATE THE MECHANISM OF BACTERIAL (M.HHAL) AND MAMMALIAN (MURINE) DNA 5-C METHYLTRANSFERASE SOL NCI-RFQ-00127-NV DUE 061200 POC Debbie Moore, Purchasing Agent (301) 402-4509, Todd Cole, Contracting Officer (301) 402-4509 The National Cancer Institute(NCI), Division of Basic Sciences (DBS), Laboratory of Medicinal Chemistry (LMC) plans to procure the services of ASH Stevens, Inc., 5861 John C. Lodge Fwy., Detroit, MI 48202 to produce optically active (+)- (benzyloxymethyl)cyclopent-3-en-1-ol. The LMC has an ongoing study for the synthesis of phosphoramidites of conformationally locked carbocyclic nucleosides to elucidate the mechanism of bacterial (M Hhal) and mammalian (Murine) DNA 5-C methyltransferase. The purpose of this investigation is to study the active or passive nature of the mechanism of base flipping, a key step during the methylation of DNA by methyltransferases. This specific project requires optically active intermediate [(+)- (benzyloxymethyl)cyclopent-3-en-1-ol] for the synthesis of the modified phosphoramidites that are necessary for the synthesis of the DNA pieces used in this investigation. ASH Stevens, under a previous competitive contract (# CM-67238), was assigned to the project to investigate the large scale synthesis of (+)-(benzyloxymethyl)cyclopent 3- en-1-ol. The successful outcome of the investigation by ASH Stevens provided the LMC with enough investigational material for startup and implementation of the aforementioned project. The LMC requires the same material previously used in the overall investigation. This will guarantee that no change in variables has occurred that could delay or even compromise the results of the study. ASH Stevens Inc. has provided an initial batch of pure (99.5 %), optically active (+) (benzyloxymethyl)cyclopent-3-en-1-ol. This successful synthesis was the result of more than a year of investigation and development. There is no other source known by the NCI researcher that has synthesized optically active (+)- (benzyloxymethyl)cyclopent-3-en-1-ol with the noted level of purity and in the amounts required for the remainder of the overall study (400-500 g) . A change in the source of this delicate material may jeopardize the success of the project by introducing changes and variables. Based on the above information, ASH Stevens is the only source known to the NCI researcher that can provide this material. This is not a request for competitive quotation. However, if any interested party believes it can perform the above requirement, it may submit a statement of capabilities. The statement of capabilities and any other information furnished must be in writing and must contain material in sufficient detail to allow NCI to determine if the party can perform this requirement without compromising the integrity of the ongoing study. Capability statements must be received in the contracting office by 2:00 PM EDT, on June 12, 2000. If you have any questions, please contact Debbie Moore, Purchasing Agent on (301) 402-4509. A determination by the Government not to compete this proposed requirement based upon responses to this notice is solely within the discretion of the Government. Information received will be considered solely for the purpose of determining whether to conduct a competitive procurement. Posted 05/24/00 (W-SN458115). (0145)

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