- PYRIDINE-1-OXIDE DERIVATIVES AND THEIR USE AS FACTOR XIA INHIBITORS
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The present invention provides a compound of Formula (I) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma kallikrein.
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Page/Page column 55
(2018/03/25)
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- Synthesis and rearrangement of [1,1′-bicyclobutyl]-1-ols and spiro[3.4]octan-5-ols: A general access to bicyclo[3.3.0]octenes (hexahydropentalenes)
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Several new Grignard reagents based on substituted cyclobutanes have been generated and added to cyclobutanones to yield mono- to trimethylated [1,1′-bicyclobutyl]-1-ols. Mono- to trimethylated spiro[3.4]octan-5-ols have been prepared from the parent ketone via alkylation and/or addition reactions. Upon treatment with acid, all [1,1′-bicyclobutyl]-1-ols and spiro[3.4]octan-5-ols rearrange to yield a single bicyclo[3.3.0]octene. Mono- to trimethylated [1,1′-bicyclobutyl]-1-ols and spiro[3.4]octan-5-ols have been synthesized and rearranged to yield a single bicyclo[3.3.0]octene in each case. Examples are 42, 43, 44 and 45.
- Mandelt, Klaus,Meyer-Wilmes, Imelda,Fitjer, Lutz
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p. 11587 - 11595
(2007/10/03)
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- Synthesis, Resolution, and Absolute Stereochemistry of (1R,2S)-(+)-cis-1-Methoxycarbonyl-2-methylcyclobutane
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Racemic cfs-1-methoxycarbonyl-2-methylcyclobutane uncontaminated with the trans isomer was prepared efficiently in five steps; the corresponding amides from (R)-(-)-phenylglycinol were separated. An X-ray crystallographic structure determination of the amide from (+)-cis-1-methoxycarbonyl-2-methylcyclobutane showed that it was of (1R,2S) absolute stereochemistry, a revision of configurational assignment.
- Baldwin, John E.,Burrell, Richard C.
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p. 7139 - 7144
(2007/10/03)
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- General Synthesis of Methyl- and Dimethyl-cyclobutanes from Simple 1,3-Diols by Phase Transfer Catalysis
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A general method is described for the preparation of methyl- and dimethyl-cyclobutanes from simple 1,3-diols.The key steps of the procedure are a phase transfer catalysed ring closure and the transformation of a carboxyl group to a methyl group.Phase transfer catalysis provides good yields in the synthesis of the cyclobutane skeleton.
- Toeroek, Bela,Molnar, Arpad
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p. 801 - 804
(2007/10/02)
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