Many dihydropyrimidinones and their derivatives play an important role in medicine due to their therapeutic and pharmacological properties. [1] They have emerged as the integral backbones of several calcium channel blockers, antihypertensive agents, alpha-1α-antagonists. [2] Strategies for the synthesis of dihydropyrimidinone nucleus have varied from one-pot to multistep approaches. Although high yields can be achieved by the following complex multistep procedures, these methods lack the simplicity comparing with Biginelli protocol which firstly reported by Biginelli by one-pot condensation of aryl aldehyde, β-ketoesters and urea with catalytic acid in 1993, and these multistep methods suffer from low yields particularly for substituted aromatic aldehyde.……
Pentaerythritol diacetals are useful in many fields. They can be applied as plasticizers and vulcanizers of various polymeric materials, as raw materials for production of valuable resins and lacquers, as physiologically active substances and as defoamers for washing solution containing anionic surfactants. [ 1 ～ 4] Synthsis of diacetals from 2,2bis(hydroxymethyl)-1, 3-propanediol with aldehydes and ketones in refluxing toluene using ZrO2/S2O2- 8 solid superacid as catalyst in 85% ～ 99% yields has been described. The catalysts are easily regenerated by washing with ethanol followed by drying at 120 ℃ for 4 h and could be reused 5 times for the synthesis pentaerythritol diacetal 3e without significant loss of activity. This method possesses the advantages of the operational simplicity, short reaction time, use of inexpensive materials, non-corrosion, non-polluting, high yields and reusable catalysts.……
JIN Tong-Shou YANG Mi-Na FENG Guo-Liang LI Tong-Shuang
