6283-71-2Relevant articles and documents
Synthesis and differential functionalisation of pyrrolidine and piperidine based spirodiamine scaffolds
Weinberg, Kamil,Stoit, Axel,Kruse, Chris G.,Haddow, Mairi F.,Gallagher, Timothy
, p. 4694 - 4707 (2013/07/04)
The synthesis and differential substitution/protection of a series of spirodiamine scaffolds are described. Methods for selective access to the two mono-N-methyl isomers based on 2,7-diazaspiro[4.5]decane are also described. Key precursors associated with this chemistry are prone to rearrangement and methods for circumventing this issue are reported. While direct mono-carbamoylation (Boc) was not efficient, selective deprotection of doubly Boc-protected derivatives derived from symmetrical diamines provided mono-Boc variants. N-Arylation, exemplified by a series of monosubstituted spirodiamines incorporating the 2-chloro-5-pyridyl moiety, which is a privileged nicotinic agonist substructure, has also been carried out to provide monoarylated secondary and tertiary spirodiamines variants.
SUBSTITUTED ARYLPYRAZOLES
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Page/Page column 75, (2010/11/25)
This invention relates to a range of C4 substituted aryl pyrazoles of Formula (I) including those 1-arylpyrazoles in which the 4-position is substituted with an acyclic substituent, a cycloalkyl ring structure or heterocyclic ring structure and which comp