A method for producing aromatic amino compound (V):
1
by synthesizing intermediate compound (IV):
2
by the reaction of compound (I): H
2
N—R
1
with a mixture of halogenated aryl compounds (II): Ar
1
-X and (III): Ar
2
-X in the presence of a noble metal catalyst, followed by eliminating the substituent R
1
from the nitrogen atom in compound (IV) under an acidic condition or an alkaline condition or by addition of a reducing agent or an oxidizing agent. (R
1
: a substituent having 2 to 50 carbon atoms; Ar
1
and Ar
2
: a substituted or unsubstituted hydrocarbon group or heterocyclic group having 6 to 50 carbon atoms and the same with or different from each other; and X: a halogen group). The aromatic amino compound useful as the charge transporting material can be produced efficiently at a great yield without using highly toxic raw materials.
[EN] PROCESS FOR THE PREPARATION OF AN (HETERO)ARYLAMINE<br/>[FR] PROCEDE DE PREPARATION D'UNE (HETERO)ARYLAMINE
申请人:DSM IP ASSETS BV
公开号:WO2006009431A1
公开(公告)日:2006-01-26
The present invention relates to a process for the preparation of an (hetero)arylamine, wherein an optionally substituted (hetero)aromatic bromide compound is contacted with a nucleophilic organic nitrogen-containing compound in the presence of a base, and a catalyst comprising a copper atom or ion and at least one ligand, said ligand comprising at least one coordinating oxygen atom, and if said oxygen atom is part of an OH group, then said OH group is attached to an aliphatic spa carbon atom or to a vinylic carbon atom.
The present invention relates to metalloprotein inhibitors comprising: a. an organic substituent and at least one zinc binding group (ZBG) covalently attached thereto; or
b. a ZBG substituted by a side chain wherein the ZBG is of formula (I):
wherein X is O or S and each R
1
, R
2
, R
3
, and R
4
is individually hydrogen or an organic radical. The metalloprotein inhibitors are useful for preventing or treating a pathological disease, condition, or symptom that is associated with pathological metalloprotein activity and/or that is alleviated by inhibition of said activity.
A method for producing aromatic amino compound (V):
by synthesizing intermediate compound (IV):
by the reaction of compound (I): H
2
N—R
1
with a mixture of halogenated aryl compounds (II): Ar
1
—X and (III): Ar
2
—X in the presence of a noble metal catalyst, followed by eliminating the substituent R
1
from the nitrogen atom in compound (IV) under an acidic condition or an alkaline condition or by addition of a reducing agent or an oxidizing agent. (R
1
: a substituent having 2 to 50 carbon atoms; Ar
1
and Ar
2
: a substituted or unsubstituted hydrocarbon group or heterocyclic group having 6 to 50 carbon atoms and the same with or different from each other; and X: a halogen group). The aromatic amino compound useful as the charge transporting material can be produced efficiently at a great yield without using highly toxic raw materials.
一种生产芳香族氨基化合物(V)的方法:
通过合成中间体化合物 (IV):
通过化合物(I)的反应H
2
N-R
1
与卤代芳基化合物 (II) 的混合物发生反应:Ar
1
-X和(III):Ar
2
-X,然后消除取代基 R
1
在酸性或碱性条件下,或通过添加还原剂或氧化剂,从化合物 (IV) 中的氮原子上消除取代基 R 1。(R
1
:具有 2 至 50 个碳原子的取代基;Ar
1
和 Ar
2
X:卤素基团)。作为电荷传输材料的芳香族氨基化合物可以在不使用剧毒原料的情况下高效生产,产量高。
Electrochemical Benzylic C–H Amination via <i>N</i>-Aminopyridinium
protocol for benzylic C(sp3)–H aminopyridylation via direct C–H/N–H cross-coupling of alkylarenes with N-aminopyridinium triflate has been developed. This method features excellent site-selectivity, broad substrate scope, redox reagent-free and facile scalability. The generated benzylaminopyridiniums can be readily converted to benzylamines via electroreductive N–N bondcleavage.