PRODUCTION OF NON NATURALLY OCCURRING AMINO ACIDS

描述（来自申请人摘要的逐字描述）：非天然存在 氨基酸，沿着其他手性含胺化合物，是一种快速的 不断增长的医药中间体类别。组合合成 这些策略常规地使用从非天然存在的 氨基酸和胺，产生了对制备这些化合物的方法的迫切需要。 研究数量的化合物。随着候选药物通过测试， 临床开发，所需的量增加。该提案的重点是 开发用于生产非天然的 存在的氨基酸。这个过程是一个手性合成，而不是一个决议， 从而有效利用碳并减少浪费。高化学产率可以 可以从简单、廉价的前体中获得。驱动方法 完成的反应将在四个目标上展示， 具有直接商业应用的天然氨基酸。的吸引 该方法的特征是其适用于宽范围的氨基酸， 胺和可以获得的高度立体化学纯度。在 除了非天然存在的氨基酸，该技术将被应用于 并评价β-氨基酸、γ-氨基酸和 手性胺，在水性和非水性介质中。最后 光学纯N-15标记氨基酸的立体选择性生产将是 演示。 拟议商业应用：不可用

DESCRIPTION (Verbatim from the applicant's abstract): Non-naturally occurring amino acids, along with other chiral amine-containing compounds, are a rapidly growing class of pharmaceutical intermediates. Combinatorial synthesis strategies routinely employ libraries prepared from non-naturally occurring amino acids and amines, creating an immediate need for methods to prepare these compounds in research quantities. As drug candidates move through testing and clinical development, the amounts needed increase. This proposal focuses on the development of a transamination process for the production of non-naturally occurring amino acids. The process is a chiral synthesis, not a resolution, leading to efficient use of carbon and reduced waste. High chemical yields can be achieved from simple, inexpensive precursors. A method for driving the reaction to completion will be demonstrated on four target non-naturally occurring amino acids having immediate commercial applications. The attractive features of the method are its applicability to a broad range amino acids and amines and the high degree of stereochemical purity that can be obtained. In addition to non-naturally occurring amino acids, the technology will be applied and evaluated for the production of beta-amino acids, gamma amino acids, and chiral amines, both in aqueous and non-aqueous media. Finally, the stereoselective production of optically pure N-15 labeled amino acids will be demonstrated. PROPOSED COMMERCIAL APPLICATION: NOT AVAILABLE