Konishi Hideyuki, Sekino Tomoyuki, Manabe Kei
School of Pharmaceutical Sciences, University of Shizuoka.
Chem Pharm Bull (Tokyo). 2018 May 1;66(5):562-567. doi: 10.1248/cpb.c18-00042. Epub 2018 Feb 14.
A practical Pd-catalyzed carbonylation of (hetero)aryl bromides using a crystalline carbon monoxide (CO) surrogate, 2,4,6-trichlorophenyl formate (TCPF), was developed. This reaction proceeds without the slow addition technique that was previously required and with a low catalyst loading (1 mol%). The utility of this Pd-catalyzed external-CO-free carbonylation using TCPF was demonstrated in the synthesis of a histone deacetylase inhibitor.
开发了一种实用的钯催化(杂)芳基溴化物的羰基化反应,该反应使用结晶一氧化碳(CO)替代物2,4,6-三氯苯基甲酸酯(TCPF)。该反应无需先前所需的缓慢添加技术,且催化剂负载量低(1 mol%)。使用TCPF的这种钯催化无外部CO羰基化反应的实用性在组蛋白去乙酰化酶抑制剂的合成中得到了证明。