Development of a Practical Synthesis of a Farnesyltransferase Inhibitor,Organic Process Research & Development

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Development of a Practical Synthesis of a Farnesyltransferase Inhibitor
Organic Process Research & Development ( IF 3.1 ) Pub Date : 2018-10-29 00:00:00 , DOI: 10.1021/acs.oprd.8b00307
Zhongping Shi ₁ , Junying Fan ₁ , David R. Kronenthal ₁ , Boguslaw M. Mudryk ₁

Affiliation

The development of a new and practical synthesis for a farnesyltransferase inhibitor 1 is described. The new route started from 2-nitro-5-cyanotoluene (9) and afforded desired 1 in eight chemical transformations. The key step involved formation of sulfonamide 13 from a hindered β-hydroxyamine 12 through an in situ protection of the hydroxyl group by forming TMS ether. Ultimately, this new route was successfully demonstrated to generate >10 kg of API in 29% overall yield.

中文翻译：

法尼基转移酶抑制剂的实用合成的发展。

描述了法呢基转移酶抑制剂1的新的实用合成方法的开发。新路线从2-硝基-5-氰基甲苯（9）开始，并在八次化学转化中获得所需的1。关键步骤涉及通过形成TMS醚原位保护羟基，由受阻的β-羟胺12形成磺酰胺13。最终，该新路线成功地证明可产生> 10 kg的API，总收率达29％。

更新日期：2018-10-29

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