Department of Physical Chemistry , University of Debrecen , P.O. Box 400, Debrecen H-4002 , Hungary.
MTA-DE Redox and Homogeneous Catalytic Reaction Mechanisms Research Group , University of Debrecen , P.O. Box 400, Debrecen H-4002 , Hungary.
J Org Chem. 2018 Dec 21;83(24):15486-15492. doi: 10.1021/acs.joc.8b02340. Epub 2018 Dec 5.
With use of a Pd(II)-sulfosalan complex as a water-soluble catalyst, we have developed an efficient synthesis of biaryls via Suzuki-Miyaura cross-coupling in water under aerobic conditions. The water-insoluble target molecules were isolated by simple filtration in analytical purity after washing with 0.01 M aqueous HCl (20 examples). In most cases, palladium contamination was below 5 ppm considered acceptable for active pharmaceutical ingredients. The established method is scalable, reproducible, and provides biaryl products in isolated yields up to 91%.
使用 Pd(II)-磺酰基丙氨酸配合物作为水溶性催化剂，我们在有氧条件下开发了一种在水中通过 Suzuki-Miyaura 交叉偶联高效合成联芳烃的方法。将目标产物用水和 0.01 M 盐酸（20 个例子）简单过滤洗涤后，以分析纯的形式通过简单过滤分离得到不溶于水的产物。在大多数情况下，钯的污染低于 5 ppm，这被认为是可接受的用于活性药物成分。该方法具有可扩展性、重现性，并能以高达 91%的分离收率得到联芳烃产物。
