New and convergent synthesis of saflufenacil,Journal of Heterocyclic Chemistry

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New and convergent synthesis of saflufenacil
Journal of Heterocyclic Chemistry ( IF 2.0 ) Pub Date : 2019-12-09 , DOI: 10.1002/jhet.3757
Bin Wang ₁ , Yongjun Mao ₁ , Xiangyu Liu ₁ , Zhiwei Zhao ₁ , Lehao Bu ₁ , Han Wang ₁

Affiliation

A new, practical, and hundred‐gram scale synthesis of saflufenacil, a protoporphyrinogen oxidase (PPO) inhibitor herbicide, is described. The key intermediate N‐methyl‐N‐isopropyl sulfamide (12) is obtained from sulfuryl chloride isocyanate, t‐butanol, and N‐methyl‐N‐isopropylamine in 74.8% yield over 3 steps. Saflufenacil is prepared in 48.6% yield over 8 steps and 98.7% purity (HPLC).

中文翻译：

新的和会聚的氨苯磺胺合成

本文描述了一种新的，实用的，百克级合成的氨苯磺草胺（一种原卟啉原氧化酶（PPO）抑制剂除草剂）。关键的中间体N-甲基-N-异丙基磺酰胺（12）是从异氰酸硫酰氯，叔丁醇和N-甲基-N-异丙基胺中分3步获得的，产率为74.8％。以8个步骤的产率为48.6％，纯度为98.7％（HPLC）制备的沙氟芬那。

更新日期：2019-12-11

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