不对称的合成β,β-异位阿兰因通过一个顺序的C-C交叉合-化策略
David A Petrone1, Jonathan Maturano2, James Herbort1
1Department of Process Research & Development, Merck & Co., Inc., MRL, Rahway, New Jersey 07065, United States.
Organic letters
|July 11, 2024
概括
我们开发了一种新方法来合成有价值的β,β-非替代氨酸衍生物. 这种高效的过程产生了具有高反选择性的多种化合物,在合成中非常有用.
科学领域:
- 有机化学 有机化学
- 合成化学 合成化学
背景情况:
- 奇拉氨基酸是制药和材料科学中的关键组成部分.
- 非蛋白质生成氨基酸的有效合成,如β,β-非替代的氨酸,仍然是一个合成的挑战.
研究的目的:
- 开发一种新型的合成策略,用于获取多种β,β-非替代氨酸衍生物.
- 为了在这些有价值的化合物的合成中实现高产量和酶选择性.
主要方法:
- 顺序C(sp2) -C(sp3) 苏苏基交叉合,然后进行不对称的化.
- 证明广泛的功能组耐受性.
- 转换成十克数量的可扩展性.
主要成果:
- 成功合成β-基-β-基和β,β-二基氨酸衍生物.
- 对目标化合物实现了高产量和优异的抗选择性.
- 适合固相合成 (SPPS) 的Fmoc氨基酸衍生物的生成.
结论:
- 开发的顺序的苏苏基合-不对称化策略可有效地获得有价值的β,β-非替代氨酸衍生物.
- 这种方法提供了广泛的功能组耐受性和可扩展性.
- 由此产生的氨基酸衍生物适用于SPPS.
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