Palladium-Catalyzed Hydroaminocarbonylation of Alkenes with Amines: A Strategy to Overcome the Basicity Barrier Imparted by Aliphatic Amines
作者:Guoying Zhang、Bao Gao、Hanmin Huang
DOI:10.1002/anie.201502405
日期:2015.6.22
A novel and efficient palladium‐catalyzed hydroaminocarbonylation of alkenes with aminals has been developed under mild reaction conditions, and allows the synthesis of a wide range of N‐alkyl linear amides in good yields with high regioselectivity. On the basis of this method, a cooperative catalytic system operating by the synergistic combination of palladium, paraformaldehyde, and acid was established
The weak acid has been identified as an efficient basicity-mask to overcome the basicitybarrierimparted by aliphaticamines in the Pd-catalyzed hydroaminocarbonylation, which enables both aromatic and aliphaticamines to be applicable in the palladium-catalyzedhydroaminocarbonylation reaction. Notably, by using this protocol, the marketed herbicide of Propanil and drug of Fentanyl could be easily
Penetration enhancers for transdermal delivery of systemic agents
申请人:WHITBY RESEARCH, Inc.
公开号:EP0268220A2
公开(公告)日:1988-05-25
This invention relates to a method for administering systemically active agents including therapeutic agents through the skin or mucosal membranes of humans and animals in a transdermal device or formulation comprising topically administering with said systemic agent an effective amount of a membrane penetration enhancer having the structural formula
wherein R¹ and R² are independently selected from the group consisting of alkyl radicals and cycloalkyl radicals comprising from 1 to 20 carbon atoms and R is selected from the group consisting of alkyl radicals and cycloalkyl radicals comprising from 1 to 30 carbon atoms; provided, however, that the total number of carbon atoms in said compound is 15 or more and the total number of carbon atoms in R¹ and R² is 5 or more.