Transition Metal‐Free, Free‐Radical Sulfenylation of the α‐C(
<i>sp</i>
<sup>3</sup>
)−H Bond in Arylacetamides and Its Application Toward 2‐Thiomethyl Benzoxazoles Synthesis
作者:Shanghui Tian、Chaoli Wang、Jianhui Xia、Jie‐Ping Wan、Yunyun Liu
DOI:10.1002/adsc.202100816
日期:2021.10.5
This paper reports the transition metal-free C(sp3)−H sulfenylation of arylacetamides by using thiophenols as the sulfenyl reagents. The reactions take place in the presence of only K3PO4. Control experiments indicate that the reactions proceed via a featured sulfur-centred free radical intermediate. In addition, the synthesis of 2-thiomethyl benzoxazoles has been realized via the p-toluenesulfonic
本文报道了使用苯硫酚作为亚苯基试剂对芳基乙酰胺进行无过渡金属的 C( sp 3 )-H 亚苯基化反应。反应仅在 K 3 PO 4存在下发生。对照实验表明反应通过以硫为中心的自由基中间体进行。此外,2-硫甲基苯并恶唑的合成是通过对甲苯磺酸(p- TSA)促进的苯磺酰化产物的环化实现的。
Tunable Single and Double γ‐C−H Arylation of Phenylacetamides Directed by
<i>o</i>
‐Aminophenols
作者:Zhi Tu、Yi Du、Xiaoji Cao、Yunyun Liu
DOI:10.1002/adsc.201900866
日期:2019.11.5
available o‐aminophenols (OAPs) have been identified as practical directing component for the Pd‐catalyzed aromatic γ‐C−H bond arylation of phenylacetamides. Notably, the selective single and double arylation of the C−H bond(s) in the γ‐potion has been independently realized by simply modifying reaction conditions. The catalytic system of Pd(CF3OO)2/K2S2O8/K2CO3 enables the selective single C−H arylation
廉价且容易获得的邻氨基苯酚(OAP)已被确定为苯乙酰胺在Pd催化的芳族γ-C-H键芳基化反应中的实际指导成分。值得注意的是,通过简单地修改反应条件就可以独立地实现γ部分中CH键的选择性单芳基化和双芳基化。Pd(CF 3 OO)2 / K 2 S 2 O 8 / K 2 CO 3的催化体系能够实现选择性的单一CH芳基化。另一方面,在KIO 3 / K 2 CO 3存在下催化Pd(OAc)2 诱导两个γ-C-H键的选择性芳基化。
Benzoxazoles
申请人:Euro-Celtique, S.A.
公开号:US06372770B1
公开(公告)日:2002-04-16
Novel compounds which are effective PDE IV inhibitors are disclosed. The compounds possess improved PDE IV inhibition as compared to theophylline or rolipram, with improved selectivity with regard to, e.g., PDE III inhibition.