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Scale-Up Investigation of Aggarwal Enal Bicyclic Intermediate Synthesis
Organic Process Research & Development ( IF 3.1 ) Pub Date : 2024-06-18 , DOI: 10.1021/acs.oprd.4c00209
Andrejs Pelšs 1 , Kirill Shubin 1
Affiliation  

Recently, a multitude of modern and short syntheses of various prostanoids were reported, rejuvenating this synthesis field. One such synthesis reported by Aggarwal et al. has good potential for industrialization. Herein, synthesis of bicyclic enal intermediate (Aggarwal enal) was demonstrated on a hectogram scale by finding an appropriate l-proline source which is soluble under overhead stirring conditions in reactor. Kilogram scale synthesis of volatile starting material─succinaldehyde─was achieved in a high yield by finding a suitable isolation method.

中文翻译:


Aggarwal Enal 双环中间体合成的放大研究



最近,报道了各种前列腺素类化合物的大量现代和短合成,使该合成领域焕发了活力。 Aggarwal 等人报道了一种这样的合成。具有良好的产业化潜力。在此,通过寻找在反应器顶部搅拌条件下可溶的合适的L-脯氨酸源,以百克规模演示了双环烯醛中间体(Aggarwal enal)的合成。通过寻找合适的分离方法,以高产率实现了公斤级规模的挥发性原料琥珀醛的合成。
更新日期:2024-06-18
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