- A practical synthesis of m-prostaglandin E synthase-1 inhibitor MK-7285
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(Chemical Equation Presented) A practical, kilogram-scale chromatography-free synthesis of mPGE synthase I inhibitor MK-7285 is described. The route features a convergent assembly of the core phenanthrene unit via amide-directed ortho-metalation and proxi
- Gosselin, Francis,Lau, Stephen,Nadeau, Christian,Trinh, Thao,O'Shea, Paul D.,Davies, Ian W.
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scheme or table
p. 7790 - 7797
(2010/03/05)
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- PROCESSES FOR PREPARATION OF CYCLOPROPYLETHANOL, CYCLO-PROPYLACETONITRILE AND INTERMEDIATES OF BOTH
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A process for preparation of cyclopropylethanol, which comprises subjecting a 3-cyclopropyl-2,3-epoxypropionic acid ester to solvolysis, treating the product of the solvolysis with an acid to obtain cyclopropylacetaldehyde, and reducing the obtained cyclopropylacetaldehyde; and a process for preparation of cyclopropylacetonitrile, which comprises subjecting a 3-cyclopropyl-2,3-epoxypropionic acid ester to solvolysis in the presence of a base, treating the product of the solvolysis with an acid to obtain cyclopropylacetaldehyde, reacting the obtained cyclopropylacetaldehyde with hydroxylamine or salts thereof to obtain cyclopropaneacetaldehyde oxime, and reacting the obtained cyclopropaneacetaldehyde oxime with acetic anhydride. According to the present invention, cyclopropylethanol and cyclopropylacetonitrile can be prepared at low costs and industrially advantageously.
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- 2-Ureido-thiazole derivatives, process for their preparation, and their use as antitumor agents
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Compounds which are 2-ureido-1,3-thiazole derivatives of formula (I) wherein R is a halogen atom, a nitro group, an optionally substituted amino group or it is a group, optionally further substituted, selected from: i) straight or branched C1-C6 alkyl; ii) C3-C6 cycloalkyl; iii) aryl or arylalkyl with from 1 to 6 carbon atoms within the straight or branched alkyl chain; R1 is an optionally substituted group selected from: i) straight or branched C1-C6 alkyl; ii) 3 to 6 membered carbocycle or 5 to 7 membered heterocycle ring, iii) aryl or arylcarbonyl; iv) arylalkyl with from 1 to 6 carbon atoms within the straight or branched alkyl chain: R2 is hydrogen, a straight or branched C1-C4 alkyl or C2-C4 alkenyl or alkynyl group; or, taken together with the nitrogen atom to which they are bonded, R1 and R2 form a substituted or unsubstituted group selected from: i) an optionally benzocondensed or bridged 5 to 7 membered heterocycle; or ii) a 9 to 11 membered spiro-heterocyclic compound; or a pharmaceutically acceptable salt thereof; are useful for treating cell proliferative disorders associated with an altered cell dependent kinase activity.
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- METHOD FOR TREATING ANXIETY
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The present invention provides a method for treating anxiety in humans using azacyclic or azabicyclic compounds.
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- HETEROCYCLIC COMPOUNDS AND THEIR PREPARATION AND USE
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The present invention relates to therapeutically active azacyclic or azabicyclic compounds, a method of preparing the same and to pharmaceutical compositions comprising the compounds. The novel compounds are useful in treating diseases in the central nervous system caused by malfunctioning of the muscarinic cholinergic system.
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- 22-Hydroxycholesterol Derivatives as HMG CoA Reductase Suppressors and Serum Cholesterol Lowering Agents
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A series of 22-hydroxycholesterol derivatives with a modified side chain terminus was prepared.These agents were evaluated in vitro and in vivo for their ability to suppress HMG CoA reductase, the rate-limiting enzyme of cholesterol biosynthesis.In tissue culture assays, 22-hydroxycholesterol as well as the side chain modified analogues were potent inhibitors of HMG CoA reductase.However, only those sterols with a modified side chain terminus were effective suppressors of liver reductase whene administered ig to rats. 22-Hydroxy-25-methylcholesterol (4a) and 25-fluoro-22-hydroxycholesterol (15a) significantly lowered serum cholesterol levels when administered ig to primates; 25-chloro-22-hydroxycholesterol (15b) and the analogue with a cyclopropyl terminus, 20b, were ineffective.The cholesterol-lowering sterols did not significantly alter lipoprotein levels; however, the two compounds have been shown to inhibit acyl-coenzyme A:cholesterol-transferase (ACAT) in tissue culture studies
- Chorvat, Robert J.,Desai, Bipin N.,Radak, Suzanne Evans,McLaughlin, Kathleen T.,Miller, James E.,et al.
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p. 194 - 200
(2007/10/02)
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- Pyridine esters of cyclopropane-carboxylic acid
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Heterocyclic organic esters and thioesters characterized by the presence of one or two cyclopropane moieties, synthesis thereof, and compositions thereof for the control of mites and ticks.
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- Control of Acarina by esters of cyclopropane acids
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Methods and compositions for the control of Acarina employing esters of cyclopropane carboxylic acids described herein.
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