当前位置： SCI文献检索 > ACS Combinatorial Science期刊下所有文献 > Application of sequential Cu(I)/Pd(0)-catalysis to solution-phase parallel synthesis of combinatorial libraries of dihydroindeno[1,2-c]isoquinolines.

Application of sequential Cu(I)/Pd(0)-catalysis to solution-phase parallel synthesis of combinatorial libraries of dihydroindeno[1,2-c]isoquinolines.

Abstract：

:Parallel solution-phase synthesis of combinatorial libraries of dihydroindenoisoquinolines employing a sequential Cu(I)/Pd(0)-catalyzed multicomponent coupling and annulation protocol was realized. The scope and limitations of the protocol with respect to the substitution pattern in the aryl ring of the indene core, as well as the N-substituent have been defined, revealing that the methodology is compatible with a wide-range of aliphatic linear, branched, and ester functionalized N-substituents. Unexpectedly, the formation of regioisomers featuring a 1,2,3-contiguous substitution pattern in the aromatic ring of the indene core was observed. Three distinct combinatorial libraries with a total of 111 of members were synthesized, and 80 highly substituted dihydroindenoisoquinolines structurally related to known medicinal agents including some consisting of mixtures of two regioisomers were made available for biological activity testing.

journal_name

ACS Comb Sci

journal_title

ACS combinatorial science

authors

Kumar S,Painter TO,Pal BK,Neuenswander B,Malinakova HC

doi

10.1021/co200027c

subject

Has Abstract

pub_date

2011-09-12 00:00:00

pages

466-77

issue

5

eissn

2156-8952

issn

2156-8944

journal_volume

13

pub_type

杂志文章

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