Controlled photo-flow oxidative reaction (UV-FOR) platform for ultra-fast phthalide and API synthesis,Green Chemistry

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Controlled photo-flow oxidative reaction (UV-FOR) platform for ultra-fast phthalide and API synthesis
Green Chemistry ( IF 9.3 ) Pub Date : 2018-09-12 , DOI: 10.1039/c8gc02320d
Dnyaneshwar Aand _{1,

2,

3,

4} , Sanjeev Karekar _{1,

2,

3,

4} , Bhushan Mahajan _{1,

2,

3,

4} , Amit B. Pawar _{1,

2,

3,

4} , Ajay K. Singh _{1,

2,

3,

4}

Affiliation

An integrated photo-flow oxidative reaction (UV-FOR) platform approach is presented for the synthesis of phthalides. The current protocol is catalyst-free, and uses economical and abundant hydro-carbons and hydrocarbon derivatives such as benzoic acid, benzene, and xylene, as starting materials. The reaction is performed using oxygen as a green oxidant in a time- and labour-efficient manner. This integrated approach has been shown to be successful in making a UV-FOR platform suitable for the on-demand synthesis of phthalides and their further syntheses to 2-arylmethylbenzoic acids and arylogous Michael addition products under relatively mild conditions. The current protocol was further extended to the gram scale synthesis of an ischemic stroke-relevant active pharmaceutical ingredient (API), 3-N-butylphthalide (NBP), in a continuous flow process.

中文翻译：

可控的光流氧化反应（UV-FOR）平台，用于超快邻苯二甲酰亚胺和API合成

提出了一种集成的光流氧化反应（UV-FOR）平台方法用于邻苯二甲酸酯的合成。当前的方案是无催化剂的，并且使用经济且丰富的烃类和烃衍生物（例如苯甲酸，苯和二甲苯）作为起始原料。使用氧气作为绿色氧化剂以省时省力的方式进行反应。事实证明，这种集成方法可以成功地制造出适合在相对温和的条件下按需合成邻苯二甲酸酯及其进一步合成为2-芳基甲基苯甲酸和迈克尔基加成产物的UV-FOR平台。目前的方案进一步扩展到缺血性卒中相关活性药物成分（API）3- N的克级合成连续流动过程中的邻苯二甲酸丁二酯（NBP）。

更新日期：2018-10-15

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