PRODUCTION OF NON NATURALLY OCCURRING AMINO ACIDS

描述(逐字摘自申请人的摘要)：非自然发生的 氨基酸和其他手性含胺化合物是一种快速的 越来越多的医药中间体。组合综合 策略通常使用非自然发生的库 氨基酸和胺，迫切需要制备这些物质的方法 研究数量的化合物。随着候选药物通过测试和 临床开发，所需的量增加。这项提案的重点是 开发一种用于生产非天然产品的转氨基工艺 出现的氨基酸。这个过程是手性合成，而不是拆分， 从而有效利用碳并减少浪费。高化学产率可以 从简单、廉价的前体就可以实现。一种驱动汽车的方法 完成后的反应将在四个目标上进行非自然演示 现成的氨基酸具有立即的商业应用。有吸引力的 该方法的特点是适用于广泛的氨基酸和 胺和可获得的高度立体化学纯度。在……里面 除了非自然产生的氨基酸外，这项技术还将被应用 并评估了β-氨基酸、伽马氨基酸和 水和非水介质中的手性胺。最后， 光学纯N-15标记氨基酸的立体选择性生产将是 演示了。 建议的商业应用：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