Custom Pharmaceutical Services, Dr Reddy's Laboratories Limited, Bollaram Road Miyapur, Hyderabad, 500 049, India.
Org Biomol Chem. 2012 Apr 21;10(15):3098-103. doi: 10.1039/c2ob25296a. Epub 2012 Mar 9.
A one-pot cascade reaction has been developed leading to the concurrent construction of six and five membered fused N-heterocyclic rings of indazolo[3,2-b]quinazolinones. The methodology involved the reaction of isatoic anhydride, a hydrazine and o-iodo benzaldehyde in the presence of Pd(PPh(3))(4) and BINAP in MeCN. The mechanism of this cascade reaction is discussed. A variety of indazolo[3,2-b]quinazolinone derivatives were prepared by using this methodology in good yields, some of which were tested for their PDE4 inhibitory properties in vitro. The dose response and docking study performed using a representative compound is presented.
已经开发出一种一锅级联反应，可同时构建六个和五个稠合的 N-杂环并喹唑啉酮的五元环。该方法涉及在 Pd(PPh(3))(4)和 BINAP 的存在下，使异邻苯二甲酰亚胺、肼和邻碘苯甲醛反应。讨论了这种级联反应的机制。通过该方法以良好的收率制备了各种吲唑并[3,2-b]喹唑啉酮衍生物，其中一些衍生物进行了体外 PDE4 抑制活性测试。呈现了使用代表性化合物进行的剂量反应和对接研究。
