Herein we report a general electrochemical strategy for the Sandmeyer reaction. Using electricity as the driving force, this protocol employs a simple and inexpensive halogen source, such as NBS, CBrCl3, CH2I2, CCl4, LiCl and NaBr for the halogenation of aryl diazonium salts. In addition, we found that these electrochemical reactions could be performed using anilines as the starting material in a one-pot
本文中,我们报告了桑德迈尔反应的一般电化学策略。使用电作为驱动力,该协议采用一种简单且廉价的卤素源,例如NBS,CBrCl 3,CH 2 I 2,CCl 4,LiCl和NaBr进行芳基重氮盐的卤化。另外,我们发现这些电化学反应可以以一锅的方式使用苯胺作为起始原料来进行。此外,该方法的实用性在使用非常便宜的石墨作为电极的多克规模的芳基卤化物的合成中得到了证明。已经进行了一系列详细的机理研究,包括自由基时钟和自由基清除剂研究,循环伏安分析和原位电子顺磁共振(EPR)分析。
Pyrimidodiazepinone derivative
申请人:Kyowa Hakko Kirin Co., Ltd.
公开号:US07998954B2
公开(公告)日:2011-08-16
The invention provides a pyrimidodiazepinone derivative represented by the general formula (I)
[wherein n represents 1 or 2, Z represents a hydrogen atom or the like, R1 and R2 may be the same or different, and each represents a hydrogen atom or the like, A represents a bond, (CH2)m (wherein m represents an integer of 1 to 4), optionally substituted phenylene, optionally substituted pyridinediyl, or C═O, R3 represents a hydrogen atom, optionally substituted lower alkyl, or the like, and R4 represents a hydrogen atom or the like], or a pharmaceutically acceptable salt thereof or the like.
A compound is represented by Structural Formula A1:
C—B-L-A A1
or a pharmaceutically acceptable salt or solvate thereof.
A is a prostate specific membrane antigen (PSMA) ligand;
L is an optionally substituted aliphatic or heteroaliphatic linking group;
B includes at least one optionally substituted moiety selected from the group consisting of a sugar, a charged group, an aryl ring, and a heteroaryl ring, wherein B optionally includes a drug or a labeling agent; and
C is H, a drug, or a labeling agent, wherein CB together comprises the drug or the labeling agent.
The compounds are useful as PSMA agents and in pharmaceutical compositions, methods for treating and detecting diseases such as cancer in a subject, methods for identifying cancer cells in a sample, methods for inhibiting tumor neovascularization, methods for identifying drugs that can treat cancer, and the like.
An object of the present invention is to provide an ultraviolet curing liquid composition having high sensitivity, excellent storage stability, low viscosity, and excellent fixability after ultraviolet curing. The ultraviolet curable liquid composition of the present invention is an ultraviolet curable liquid composition containing a cationically polymerizable liquid monomer, a photopolymerization initiator and a photopolymerization sensitizer, wherein the cationically polymerizable liquid monomer is a vinyl ether compound, the photopolymerization initiator includes a compound represented by general formula (1), and the photopolymerization sensitizer includes (A) at least one compound selected from the group consisting of a compound represented by general formula (2) and a compound represented by general formula (3), and (B) at least one compound selected from the group consisting of a compound represented by general formula (4) and a compound represented by general formula (5).