A Practical Synthesis of a cis-4,5-Bis(4-chlorophenyl)imidazoline Intermediate for Nutlin Analogues

作者：Shu Lianhe^*; Wang Ping; Liu Wen; Gu Chen

来源：Organic Process Research & Development, 2012, 16(11): 1866-1869.

DOI：10.1021/op300254q

A practical synthesis of cis-4,5-bis(4-chlorophenyl)imidazoline, a key intermediate for Nutlin analogues, is reported. The title compound was prepared in 81-88% yield by boric acid catalyzed direct condensation of meso-bis(4-chlorophenyl)ethane-1,2-diamine with a benzoic acid. The process was successfully scaled up in a pilot plant, resulting in >15 kg of the product.

• 出版日期2012-11