In this paper, we report an improved method for preparing 2--alkoxy 5 fluoro--3H --4--pyrimidone from 2--chloro--5--fluoro--3H--4--pyrimidone and sodium alkoxide under normal pressure at reflux temperature. Some new c...In this paper, we report an improved method for preparing 2--alkoxy 5 fluoro--3H --4--pyrimidone from 2--chloro--5--fluoro--3H--4--pyrimidone and sodium alkoxide under normal pressure at reflux temperature. Some new compounds were synthesized in higher yield by this method.展开更多
A series of novel pyrazole-based lipoprotein-associated phospholipase A2 （Lp-PLA2） inhibitors have been de- signed and synthetized by a variety of acetophenones via a 10-step convergent approach. The synthetic appro...A series of novel pyrazole-based lipoprotein-associated phospholipase A2 （Lp-PLA2） inhibitors have been de- signed and synthetized by a variety of acetophenones via a 10-step convergent approach. The synthetic approach is carefully optimized, and an unsuccessful alternative route is also discussed. The in vitro biological activity reveals that all the synthesized compounds are potent Lp-PLA2 inhibitors with compound 13b being the most potent one （Lp-PLA2, IC50= 1.5 nmol/L）.展开更多
基金The project is supported by Natural Science Foundation of Shandong.
文摘In this paper, we report an improved method for preparing 2--alkoxy 5 fluoro--3H --4--pyrimidone from 2--chloro--5--fluoro--3H--4--pyrimidone and sodium alkoxide under normal pressure at reflux temperature. Some new compounds were synthesized in higher yield by this method.
文摘A series of novel pyrazole-based lipoprotein-associated phospholipase A2 （Lp-PLA2） inhibitors have been de- signed and synthetized by a variety of acetophenones via a 10-step convergent approach. The synthetic approach is carefully optimized, and an unsuccessful alternative route is also discussed. The in vitro biological activity reveals that all the synthesized compounds are potent Lp-PLA2 inhibitors with compound 13b being the most potent one （Lp-PLA2, IC50= 1.5 nmol/L）.
