Dendritic polyesters bearing COOH groups at the focal points were grafted onto nanometer silica premodified with 3-aminopropyltriethoxysilane by N,N′-dicyclohexylcarbodiimide mediated amidation. The products were cha...Dendritic polyesters bearing COOH groups at the focal points were grafted onto nanometer silica premodified with 3-aminopropyltriethoxysilane by N,N′-dicyclohexylcarbodiimide mediated amidation. The products were characterized qualitatively by FTIR, TGA and elemental analysis. It was shown that a significant grafting （10%15% net grafting for this reaction） was obtained despite the steric hindrance of the dendrons.展开更多
A new synthesis of spirocyclic oxindole analogue spiro[piperidine-4,3＇-pyrrolol2,3-b]pyridin]-2＇（1＇H）-one 1 is described. The key steps involve dialkylation of arylacetonitrile and cyclization of the azaoxindole ...A new synthesis of spirocyclic oxindole analogue spiro[piperidine-4,3＇-pyrrolol2,3-b]pyridin]-2＇（1＇H）-one 1 is described. The key steps involve dialkylation of arylacetonitrile and cyclization of the azaoxindole ring by an intramolecular Buchwald-Hartwig amidation of carboxylic amide and aryl chloride. A small library was obtained by reductive amination of 1 with various aldehydes and was screened against human lung cancer cell A549, human liver cancer cell BEL7402, and human colon cancer cell HCT-8. The results show that most of the library compounds 2 have some inhibitory activities. 2-（Trifluoromethoxy） benzylic substituted spirocyclic azaoxindole 2e was identified as a nanomolar inhibitor against human lung cancer cell A-549 （IC50 = 50 nmol/L）.展开更多
以碘值135的棉油脂肪酸作为原料通过合成与复配方法获得一种新型磷矿选矿捕收剂;首先将脂肪酸与酰胺药剂进行酰胺化,然后在合成的药剂中复配一定量的烷基酚聚氧乙烯醚表面活性剂.通过气相色谱分析了该脂肪酸的组成,以贵州磷矿为对象,利...以碘值135的棉油脂肪酸作为原料通过合成与复配方法获得一种新型磷矿选矿捕收剂;首先将脂肪酸与酰胺药剂进行酰胺化,然后在合成的药剂中复配一定量的烷基酚聚氧乙烯醚表面活性剂.通过气相色谱分析了该脂肪酸的组成,以贵州磷矿为对象,利用常温浮选试验研究了该捕收剂的选矿特性.试验结果表明,碘值135脂肪酸中油酸、亚油酸含量较高,在碳链结构中双键、三键数目多.经过酰胺化和复配15%的表面活性剂烷基酚聚氧乙烯醚,提高了脂肪酸对磷酸盐矿物的浮选效果,在常温浮选过程中,降低了捕收剂的用量.在磨矿细度为-0.074 mm 79.83%,采用常温正反浮选工艺,获得了五氧化二磷为30.12%精矿,产率为71.20%,回收率为92.90%的选矿指标.展开更多
Transition-metal catalyzed C--H functionalization of benzaldehydes is of great interest in organic synthesis. Herein, we developed a transient directing group assisted amidation of benzaldehydes catalyzed by rhodium c...Transition-metal catalyzed C--H functionalization of benzaldehydes is of great interest in organic synthesis. Herein, we developed a transient directing group assisted amidation of benzaldehydes catalyzed by rhodium catalyst. With the employment of 10 mol% of 4-trifluoromethyl aniline, the in situ generated imine groups as the directing group efficiently enable this transformation. By using this protocol, a wide range of benzaldehydes were efficiently converted into the corresponding N-（2-formylphenyl）benzamides utilizing dioxazolones as the nitrogen source.展开更多
文摘Dendritic polyesters bearing COOH groups at the focal points were grafted onto nanometer silica premodified with 3-aminopropyltriethoxysilane by N,N′-dicyclohexylcarbodiimide mediated amidation. The products were characterized qualitatively by FTIR, TGA and elemental analysis. It was shown that a significant grafting （10%15% net grafting for this reaction） was obtained despite the steric hindrance of the dendrons.
基金supported by the program of research fund for returning scholars of Ministry of Education of China(No.200812)the Open Foundation of Chemical Engineering Subject(No.200903),Qingdao University of Science & Technology,China
文摘A new synthesis of spirocyclic oxindole analogue spiro[piperidine-4,3＇-pyrrolol2,3-b]pyridin]-2＇（1＇H）-one 1 is described. The key steps involve dialkylation of arylacetonitrile and cyclization of the azaoxindole ring by an intramolecular Buchwald-Hartwig amidation of carboxylic amide and aryl chloride. A small library was obtained by reductive amination of 1 with various aldehydes and was screened against human lung cancer cell A549, human liver cancer cell BEL7402, and human colon cancer cell HCT-8. The results show that most of the library compounds 2 have some inhibitory activities. 2-（Trifluoromethoxy） benzylic substituted spirocyclic azaoxindole 2e was identified as a nanomolar inhibitor against human lung cancer cell A-549 （IC50 = 50 nmol/L）.
文摘以碘值135的棉油脂肪酸作为原料通过合成与复配方法获得一种新型磷矿选矿捕收剂;首先将脂肪酸与酰胺药剂进行酰胺化,然后在合成的药剂中复配一定量的烷基酚聚氧乙烯醚表面活性剂.通过气相色谱分析了该脂肪酸的组成,以贵州磷矿为对象,利用常温浮选试验研究了该捕收剂的选矿特性.试验结果表明,碘值135脂肪酸中油酸、亚油酸含量较高,在碳链结构中双键、三键数目多.经过酰胺化和复配15%的表面活性剂烷基酚聚氧乙烯醚,提高了脂肪酸对磷酸盐矿物的浮选效果,在常温浮选过程中,降低了捕收剂的用量.在磨矿细度为-0.074 mm 79.83%,采用常温正反浮选工艺,获得了五氧化二磷为30.12%精矿,产率为71.20%,回收率为92.90%的选矿指标.
基金Acknowledgement We thank National Basic Research Program of China （973 Program） （No. 2015CB856600）, the National Natural Science Foundation of China （Nos. 21632001, 21772002）, National Young Topnotch Talent Support Program, and Peking University Health Science Center （No. BMU20160541） for financial support of this work. We thank Bencong Zhu in this group for reproducing the results of 3b and 4f.
文摘Transition-metal catalyzed C--H functionalization of benzaldehydes is of great interest in organic synthesis. Herein, we developed a transient directing group assisted amidation of benzaldehydes catalyzed by rhodium catalyst. With the employment of 10 mol% of 4-trifluoromethyl aniline, the in situ generated imine groups as the directing group efficiently enable this transformation. By using this protocol, a wide range of benzaldehydes were efficiently converted into the corresponding N-（2-formylphenyl）benzamides utilizing dioxazolones as the nitrogen source.
