Laboratoire d'Innovation Thérapeutique, Labex MEDALIS, Faculté de Pharmacie, UMR7200 CNRS , Université de Strasbourg , 74 Route du Rhin , 67412 Illkirch , France.
Org Lett. 2019 Feb 1;21(3):844-848. doi: 10.1021/acs.orglett.9b00031. Epub 2019 Jan 18.
An efficient and user-friendly palladium(II) precatalyst, POxAP (post-oxidative-addition precatalyst), was identified for use in Fukuyama cross-coupling reactions. Suitable for storage under air, the POxAP precatalyst allowed reaction between thioesters and organozinc reagents with turnover numbers of ∼90000. A series of 23 ketones were obtained with yields ranging from 53 to 99%. As proof of efficacy, an alternative approach was developed for the synthesis of a key precursor of the natural product isoprekinamycin.
一种高效、用户友好的钯（II）前催化剂 POxAP（后氧化加成前催化剂）被确定用于富山交叉偶联反应。该前催化剂适合在空气中储存，可使硫酯与有机锌试剂发生反应，周转数约为 90000。一系列 23 种酮以 53%至 99%的收率得到。作为有效性的证明，开发了一种替代方法来合成天然产物异普雷霉素的关键前体。
