An efficient, mild and transition-metal-free method for the N-arylation of acetanilides, leading to a range of unsymmetrical diarylamine products is reported. Reactions of ortho-silylaryl triflates with acetanilides in the presence of tetrabutylammonium triphenyldifluorosilicate (TBAT) in toluene afforded the desired products in good to excellent yields. Regioselectivity was also observed when unsymmetrical aryne precursors were used. (C) 2011 Elsevier Ltd. All rights reserved.
3-piperidyl-4-oxoquinazoline derivatives and pharmaceutical compositions comprising the same
申请人:Japan Tobacco, Inc.
公开号:US06235730B1
公开(公告)日:2001-05-22
3-piperidyl-4-oxoquinazoline derivatives are provided, which is represented by the formula (I):
wherein R represents an amino group or a cyclic amino group such as dibenzoazepine, each of which is substituted with a substituted or unsubstituted aryl group, a substituted or unsubstituted heteroaryl group, or the like, n is an integer of 1 to 3, R3 and R4 independently represents a hydrogen atom, a lower alkyl group, or the like, or a pharmaceutically acceptable salt thereof. Compounds (I) of the present invention have excellent MTP-inhibitory activity. Thus, these compounds not only inhibit formation of LDL that is a cause of arteriosclerotic diseases but also regulate TG, cholesterol, and lipoproteins such as LDL in the blood and regulate cellular lipids through regulation of MTP activity. They can also be used as a new type of preventive or therapeutic agents for hyperlipemia or arteriosclerotic diseases. Furthermore, they can be used as therapeutic or preventive agents for pancreatitis, obesity, hypercholesterolemia, and hypertriglyceridemia.
Exploiting the Marcus inverted region for first-row transition metal–based photoredox catalysis
作者:Amy Y. Chan、Atanu Ghosh、Jonathan T. Yarranton、Jack Twilton、Jian Jin、Daniela M. Arias-Rotondo、Holt A. Sakai、James K. McCusker、David W. C. MacMillan
DOI:10.1126/science.adj0612
日期:2023.10.13
Second- and third-row transitionmetal complexes are widely employed in photocatalysis, whereas earth-abundant first-row transitionmetals have found only limited use because of the prohibitively fast decay of their excited states. We report an unforeseen reactivity mode for productive photocatalysis that uses cobalt polypyridyl complexes as photocatalysts by exploiting Marcus inverted region behavior
第二和第三行过渡金属络合物广泛应用于光催化,而地球上丰富的第一行过渡金属由于其激发态的快速衰减而仅具有有限的用途。我们报告了一种不可预见的高效光催化反应模式,该模式利用钴聚吡啶配合物作为光催化剂,利用马库斯倒置区域行为,将激发态能量的增加与激发态寿命的增加结合起来。这些钴 (III) 配合物凭借其强大的氧化还原电位和足够长的激发态寿命可以参与双分子反应,催化氧化 C(sp 2 )–芳基酰胺与具有挑战性的位阻芳基硼酸的 N 偶联。更一般地说,结果意味着发色团可以设计为增加激发态寿命,同时增加激发态能量,为使用相对丰富的金属作为光氧化还原催化剂提供了途径。
3-PIPERIDYL-4-OXOQUINAZOLINE DERIVATIVES AND MEDICINCAL COMPOSITIONS CONTAINING THE SAME
申请人:Japan Tobacco Inc.
公开号:EP0970954A1
公开(公告)日:2000-01-12
3-piperidyl-4-oxoquinazoline derivatives are provided, which is represented by the formula (I):
wherein R represents an amino group or a cyclic amino group such as dibenzoazepine, each of which is substituted with a substituted or unsubstituted aryl group, a substituted or unsubstituted heteroaryl group, or the like, n is an integer of 1 to 4, R3 and R4 independently represents a hydrogen atom, a lower alkyl group, or the like, or a pharmaceutically acceptable salt thereof. Compounds (I) of the present invention have excellent MTP-inhibitory activity. Thus, these compounds not only inhibit formation of LDL that is a cause of arteriosclerotic diseases but also regulate TG, cholesterol, and lipoproteins such as LDL in the blood and regulate cellular lipids through regulation of MTP activity. They can also be used as a new type of preventive or therapeutic agents for hyperlipemia or arteriosclerotic diseases. Furthermore, they can be used as therapeutic or preventive agents for pancreatitis, obesity, hypercholesterolemia, and hypertriglyceridemia.