CAS: 17346-16-6; 2,4-Dibromo-2,4-Dimethylpentan-3-One

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📜2,4-二甲基-3-戊酮置于溴体系中,用 氯仿 用作溶剂,化学反应生成2,4-二溴-2,4-二甲基-3-戊酮
参考文献:Bace 抑制剂 Bi 1147560 Bs 和 Bi 1181181 Mz 的工艺开发
标题:Bace 抑制剂 Bi 1147560 Bs 和 Bi 1181181 Mz 的工艺开发
摘要:描述了两种β位淀粉样蛋白前体蛋白裂解酶 (Bace) 抑制剂的大规模合成的发展.发现了新的方法来克服现有程序的安全性和可扩展性问题.通过将氨基甲酰基阴离子添加到n-亚磺酰基酮亚胺,以高非对映选择性形成空间位阻季新戊基立构中心.芳基腈是通过不含钯和氰化物的亲电氰化反应安装的,该氰化反应受芳基镁衍生物与二甲基丙二腈的转腈作用影响.基于丙二酸二乙酯和二苄胺起始原料,设计了一条通往氧杂环丁基甲基胺侧链的安全路线.开发了一种温和的烯胺氟化反应,用于合成氟代异丁胺侧链.
Doi:10.1021/acs.Oprd.2C00325

专利信息

专利号:US-6051704-A
优先权日:1996-07-22
标题:Synthesis of macrocyclic tetraamido-N ligands
发明人：GORDON-WYLIE SCOTT W; COLLINS TERRENCE J
权利人:UNIV CARNEGIE MELLON
摘要:New synthetic methods for the preparation of macrocyclic amido-N donor ligands are provided. The primary method of the present invention involves in general only two synthetic steps. In the first step, an α or β amino carboxylic acid is allowed to react with an optimal (approximately stoichiometric) amount of an activated malonate or oxalate derivative with mild heating. Upon completion of the double coupling reaction, hydrolysis of the reaction mixture yields a diamide containing intermediate (a macro linker). In the second step, stoichiometric amounts of a diamine, preferably an orthophenylene diamine, are added to the macro linker intermediate in the presence of a coupling agent and heat. This second double coupling reaction, is allowed to proceed for a period of time sufficient to produce a macrocyclic tetraamido compound. The substituent groups on the α or β amino carboxylic acid, the malonate, and the aryl diamine may all be selectively varied so that the resulting tetraamido macrocycle can be tailored to specific desired end uses. The macrocyclic tetraamide ligand may then be complexed with a metal, such as a transition metal, and preferably the middle and later transition metals, to form a robust chelate complex suitable for catalyzing oxidation reactions.

专利号:US-6011152-A
优先权日:1996-07-22
标 题 :Synthesis of macrocyclic tetraamido-N ligands