1. Mcrowave-assisted Copper-catalyzed Suzuki Coupling Reaction;2. Synthetic Study On Quinazoline-2,4(1H,3H)Diones

Two parts of study are included in this paper:Microwave-assisted Cu catalyzed Suzuki reaction; and synthesis of quinazoline-diones.In the first part, the preparation of 5-(benzyloxy)-2-methoxyphenylboronic acid and its application in Microwave-assisted Cu catalyzed Suzuki reaction are summarized. With loow-toxicity and stability, organic boron compounds are important medical intermediates been widely used in the field of drug synthesis. For nearly a century, organic chemists have been looking for an effective synthetic method for the preparation of biphenyl compounds, while Coupling reactions are known as the most widely used method for the building of C-C bond. Through the efforts of organic chemists, the Cu catalyzed coupling reaction for the synthesis of biphenyl compounds get long-term development. And as is known, Microwave-assisted reaction has been taking an increasing proportion in organic synthesis since 1986.On the basis of this background, the synthesis of 5-(benzyloxy)-2-methoxyphenyl boronic acid and its application in Microwave-assisted Cu catalyzed Suzuki reaction were studied. The target product 5-(benzyloxy)-2-methoxyphenylboronic acid was achieved through a six-step reaction, including acetylation, bromination, deacetylation, benzyl protection, boration and debenzylation, adopting hydroquinone monomethyl ether(MEHQ) as starting material And a total yield of 30% was obtained through one-step recrystallization without isolation and purification. Then we studied Microwave-assisted Cu catalyzed Suzuki reaction adopting 5-(benzyloxy)-2-methoxyphenylboronic acid as raw material, and Cul as catalysis for the first time, and finally obtained six bis-aryl compounds.The second part concludes our research on the synthesis of quinazoline-diones. Quinazoline is a type of important heterocyclic compounds, which show various biological activities. This paper reports an eco-friendly, one-pot synthesis of quinazoline-2,4(1H,3H)-diones adopting water as solvent and processing under room temperature. As raw material, anthranlic acid were coupled with potassium cyanate to form urea and then subsequent cyclized to obtain monosodium salt of benzolyene urea in the presence of sodium hydroxyl, followed by acidification of the mixture to afford the final product quinazoline-2,4(1H,3H)-diones. In this method, we can get quinazoline-2,4(1H,3H)-diones through simple stirring and filtering and with no need of purification, which make it suitable for mass-production and industrial preparation.