Synthesis of Non-GMP Small Molecules

非 GMP 小分子的合成

• 批准号: 7824132
• 负责人: CHARLES KANE
• 金额: $ 42.06万
• 依托单位: STARKS ASSOCIATES, INC.
• 依托单位国家: 美国
• 财政年份: 2005
• 资助国家: 美国
• 起止时间: 2005-02-18 至 2010-02-17
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/7824132
• 关键词: Synthesis; Non; GMP; Small; Molecules

This contract will provide essential synthesis support for the early stages of the NCI drug development program. The compounds assigned for the synthesis originate from the Rapid Access To Intervention Development (RAID),Rapid Access to NCI Discovery Resources ( R*A*N*D) programs, and Biological Evaluation Committee recommendations NCI, DCTD's screening program. About 90% of the synthesis work involved in this contract originates from the current RAID and R*A*ND programs, originating from extramural applicants. Under the scope of the R*A*N*D program, synthesis of analogs in order to improve the potencies and pharmacodynamic properties of the lead compound where the core chemistry is either well established or unknown, also would fall within the scope of the contract. The remaining 10% of the work has originated upon the request of the Biological Evaluation Committee. In addition, the contract will be utilized to check the purity and identity of selected compounds as needed. The purity and identity of all resynthesized compounds and intermediates will be established by state-of-the-art physico-chemical methods. The quantities synthesized would vary from 200 mg to 100 grams. The overall objective of the contract will be the ¿Non-GMP¿ chemical synthesis of compounds of good purity needed for the cancer program, such as synthetic compounds prompted by the RAID and R*A*N*D programs, and compounds arising from recommendation of the Biological Evaluation Committee. The existing contract is not utilized for the synthesis of combinatorial libraries or leads resulting from such libraries. The new contract will be utilized for the purpose of synthesis of active single compound leads and their analogs using parallel synthesis methodology, as sometimes required by the R*A*N*D program Well-established chemistry will be applied to synthesize the needed target compounds and libraries. As such the contract is not research oriented to produce new science, but purposeful improvements by effectively utilizing existing methods or modifications in a cost-effective manner to accomplish the synthetic goals. Projects will be assigned, monitored and terminated consistent with the needs of the Program. The overall performance and accomplishments of the contract will be measured based on the complexities of the target compound assigned for synthesis, the responsiveness of the contractor to the needs of the program, the chosen synthetic approach (approaches), times of delivery, and both quality and quantity of the delivered compounds and cost effectiveness.

该合同将为NCI药物开发计划的早期阶段提供基本的综合支持。该合成分配的化合物源于对干预开发的快速访问（RAID），快速访问NCI发现资源（R*A*n*d）程序以及生物评估委员会建议NCI NCI，DCTD的筛查计划NCI。该合同涉及的合成工作中约有90％源自目前的突袭和R*a*nd程序，源自壁外应用。在r*a*n*d程序的范围下，合成类似物，以改善铅化合物的电位和药物特性，在该化合物中，核心化学的建立良好或未知，也将属于合同范围。其余10％的工作起源于生物评估委员会的要求。此外，合同将根据需要检查所选化合物的纯度和身份。所有重新合成化合物和中间体的纯度和身份将通过最先进的物理化学方法建立。合成的数量将从200 mg到100克不等。 合同的总体目的是``非GMP？non-GMP？取得了癌症计划所需的良好纯度化合物的化学合成，例如由RAID和RAID和R*A*n*d程序引起的合成化合物，以及由生物学评估委员会的建议引起的化合物。现有合同不用于合成组合图书馆或由此类库产生的潜在客户。新合同将用于使用平行综合方法的活性单个化合物铅及其类似物的目的，如r*a*a*n*d程序所要求的那样 建立的化学将应用于合成所需的目标化合物和库。因此，合同不是针对生产新科学的研究，而是通过以具有成本效益的方式有效利用现有方法或修改来实现合成目标来有目的的改进。项目将被分配，监控和终止与计划的需求一致。合同的总体绩效和成就将根据分配的合成目标化合物的复杂性，承包商对计划需求的响应，所选的合成方法（方法），交付时间以及已交付的化合物的质量和数量以及成本效益。