Cao Ping, Qu Junya, Burton George, Rivero Ralph A
GlaxoSmithKline Pharmaceuticals, 1250 South Collegeville Rd, Collegeville, Pennsylvania 19426, USA.
J Org Chem. 2008 Sep 19;73(18):7204-8. doi: 10.1021/jo801097v. Epub 2008 Aug 8.
A facile synthesis of 5-dialkylamino-6-aryl-(2H)-pyridazin-3-one from 5,6-dichloropyridazinone was carried out by using a palladium-catalyzed Suzuki-Miyaura cross coupling of 6-chloro-5-dialkylaminopyridazinone 1 with various arylboronic acids (3 equiv) as the key transformation. The Suzuki-Miyaura cross-coupling reaction proceeded smoothly under microwave irradiation at 135-140 degrees C for 30 min with 5 mol % of Pd catalyst in moderate to good isolated yields. The use of a CombiPhos Pd6 mixture catalyst system and a single Pd-SPhos catalyst system was evaluated.
以5,6-二氯哒嗪酮为原料，通过钯催化的6-氯-5-二烷基氨基哒嗪酮1与各种芳基硼酸（3当量）的铃木-宫浦交叉偶联反应，简便地合成了5-二烷基氨基-6-芳基-（2H）-哒嗪-3-酮，该反应作为关键转化步骤。铃木-宫浦交叉偶联反应在微波辐射下于135-140℃下，使用5 mol%的钯催化剂，反应30分钟，以中等至良好的分离产率顺利进行。对CombiPhos Pd6混合催化剂体系和单一Pd-SPhos催化剂体系的使用进行了评估。
