Zirconocene-induced cocyclisation/elimination reactions of 2-heterosubstituted 1,6-dienes and 1,6-enynes
Zirconocene-mediated cocyclisation of 2-heterosubstituted-1,6-dienes and -enynes gave zirconacycles bearing an endocyclic β-leaving group which eliminated under the reaction conditions to provide exocyclic alkylidene groups. The scope of this cyclisation/
Owen, David R.,Whitby, Richard J.
p. 2061 - 2074
(2007/10/03)
A Novel Cleavage Technique to Generate Small Molecule Compounds and Libraries via a Two-Resin System
Application of organic synthesis to solid supports has led to the successful implementation of combinatorial chemistry in the drug discovery process. This paper describes a novel use of the Hofmann elimination of tetrasubstituted amine salts on solid-phas
Ouyang, Xiaohu,Armstrong, Robert W.,Murphy, Martin M.
p. 1027 - 1032
(2007/10/03)
A case study of employing spectroscopic tools for monitoring reactions in the developmental stage of a combinatorial chemistry library
Organic synthesis on solid-phase resins requires new applications of nondestructive analytical tools to monitor the progress of reactions. Herein we describe our novel approach to validate a five-step reaction sequence on resin. We have developed a protocol list that allows us to follow reactions step-by-step using different analytical procedures in the order of increasing experiment time. Results from these various techniques for each reaction step are contrasted and compared. The key to achieve definitive analytical data for the entire reaction sequence is the combined application of more than one analytical technique.
Luo, Ying,Ouyang, Xiaohu,Armstrong, Robert W.,Murphy, Martin M.
p. 8719 - 8722
(2007/10/03)
?-Allyl palladium methodology for selective deprotection of allylamines. Practical synthesis of secondary amines
The palladium-promoted deallylation of allylamines derived from primary and secondary amines is achieved with high to quantitative yield in the presence of 2-mercaptobenzoic acid as an allyl scavenger.This method was used for the sequential cleavage of diallylamines.A synthetic application of this procedure is presented in the preparation of secondary amines from diallylamines. - Keywords: allylamine; deallylation; sequential deprotection; ?-allyl palladium complexes; 2-mercaptobenzoic acid; substitution of amines
Lemarie-Audoire, Sandrine,Savignac, Monique,Dupuis, Christophe,Genet, Jean Pierre
p. 1157 - 1166
(2007/10/03)
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