- Synthesis and differential functionalisation of pyrrolidine and piperidine based spirodiamine scaffolds
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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.
- Weinberg, Kamil,Stoit, Axel,Kruse, Chris G.,Haddow, Mairi F.,Gallagher, Timothy
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p. 4694 - 4707
(2013/07/04)
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- Substituted arylpyrazoles
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This invention relates to a range of 1-aryl-4-cyclopropylpyrazoles in which the cyclopropyl ring is substituted at the angular position, and pharmaceutically acceptable salts and solvates thereof, to compositions comprising such compounds, processes to their synthesis and their use as parasiticides.
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Page/Page column 82
(2008/06/13)
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- SUBSTITUTED ARYLPYRAZOLES
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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
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Page/Page column 75
(2010/11/25)
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- One-Pot Synthesis of cis Fixed β-Diketones of Bicycloalkanes, 2
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Starting from 2-cycloalken-1-ones 1 the substituted cis fixed β-diketones of bicycloalkanes 4 have been obtained by a combined Michael addition of α,α,ω-alkanetricarboxylates (and related species) 2 and Dieckmann cyclization of the intermediates 3.Reactions of the β-diketone system as well as modifications of the disubstituted malonate system of 4 are reported.
- Schank, Kurt,Lorig, Werner
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p. 112 - 136
(2007/10/02)
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