- TBAF-catalyzed cyclization of 6-hydroxyhex-2-ynoates and 7-hydroxyhept-2-ynoates
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Tetrabutyl ammonium fluoride (TBAF) was found to be capable of catalyzing the intramolecular hydroalkoxylation of 6-hydroxyhex-2-ynoates and 7-hydroxyhept-2-ynoates. The reaction could be used to prepare 2,5-substituted THF rings and 2,6-substituted THP rings.
- Wang, Xiao Qing,Jia, Ping Jing,Liu, Su Ping,Yu, Wei
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experimental part
p. 931 - 934
(2012/01/11)
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- AZAINDOLE GLUCOKINASE ACTIVATORS
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Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of metabolic diseases and disorders such as, for example, type II diabetes mellitus.
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- A novel synthesis of the north west portion of Lasonolide A - An anticancer macrolide using Claisen rearrangement
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A simplified analogue of Lasonolide A (C23-C35 side chain) was synthesized using Fujisawa's stereoselective variant of the Ireland Claisen ester rearrangement.
- Kar, Paramita,Rao,Nagaiah,Gurjar
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- BENZO(5,6)CYCLOHEPTA(1,2-B)PYRIDINE DERIVATIVES USEFUL FOR INHIBITION OF FARNESYL PROTEIN TRANSFERASE
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Novel compounds of formula (1.0) are disclosed. In Formula (1.0) a represents N or NO, R and R are halo, R and R are independently H or halo provided that at least one is H, X is C, CH or N, and T represents a five or six membered heterocycloalkyl ring having one or two heteroatoms selected from S or O. Also disclosed are methods of inhibiting farnesyl protein transferase and methods for treating tumor cells.
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- Intermolecular copper-catalyzed carbon-hydrogen bond activation via carbene insertion
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A series of catalysts of general formula TpXCu (TpX = homoscorpionate ligand) promote the insertion of :CHCO2Et (ethyl diazoacetate as the carbene source) into the C-H bonds of cycloalkanes and cyclic ethers in moderate to high yield. A correlation between the steric hindrance of these catalysts and the yield of the transformation has been observed. Copyright
- Diaz-Requejo, M. Mar,Belderrain, Tomas R.,Nicasio, M. Carmen,Trofimenko, Swiatoslaw,Perez, Pedro J.
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p. 896 - 897
(2007/10/03)
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- Compounds useful for inhibition of farnesyl protein transferase
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Novel compounds of the formula: are disclosed. In Formula 1.0 a represents N or NO, R1and R3are halo, R2and R4are independently H or halo provided that at least one is H, X is C, CH or N, and T represents a five or six membered heterocycloalkyl ring having one or two heteroatoms selected from S or O. Also disclosed are methods of inhibiting farnesyl protein transferase and methods for treating tumor cells.
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- A tandem ester cleavage-Michael addition reaction for the synthesis of oxygen heterocycles
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A tandem ester cleavage-Michael addition sequence has been developed for the preparation of five- and six-ring oxygen heterocycles bearing an acetic acid residue at C-2. Treatment of ethyl 6- or 7-acetyloxy-2-alkenoates with ethanolic sodium ethoxide affo
- Bunce,Bennett
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p. 1009 - 1020
(2007/10/02)
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- β-Alkoxyacrylates in radical cyclizations: Remarkably efficient oxacyle synthesis
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β-Alkoxyacrylates were found to be exceptionally efficient radical acceptors in radical-mediated intramolecular cyclizations. For example, reaction of 5-bromo-2-pentanol with ethyl propiolate, tributylstannane-mediated radical cyclization, and hydrolysis yielded (±) (cis-6-methyltetrahydropyran-2-yl)acetic acid, a known component of civet.
- Lee, Eun,Tae, Jin Sung,Lee, Chulbom,Park, Cheol Min
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p. 4831 - 4834
(2007/10/02)
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- Stereoselective Syntheses of α-Substituted Cyclic Ethers and syn-1,3-Diols
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In the presence of a catalytic amount of triphenylmethylium hexachloroantimonate or a catalyst system of antimony pentachloride, chlorotrimethylsilane and tin(II)iodide, α-substituted cyclic ethers are stereoselectively prepared from lactones by successiv
- Homma, Koichi,Takenoshita, Haruhiro,Mukaiyama, Teruaki
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p. 1898 - 1915
(2007/10/02)
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- Deacyloxy-alkylation of 2-Acyloxy-tetrahydrofurans and -tetrahydropyrans by Reformatsky Reagents
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A novel type of Reformatsky reaction between 2-acetoxytetrahydrofuran derivatives, ethyl bromoacetate, and zinc affords ethyl(2-tetrahydrofuranyl)acetates in the presence of a small amount of TiCl4; this reaction is also applicable to 2-acetoxytetrahydrop
- Hayashi, Masahiko,Sugiyama, Motoyoshi,Toba, Taketo,Oguni, Nobuki
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p. 767 - 768
(2007/10/02)
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- One-Pot Synthesis of α-Mono- and α,α-Disubstituted Cyclic Ethers from Lactones
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α-Mono- and α,α-disubstituted cyclic ethers are prepared in good yields by the successive treatment of lactones with t-butyldimethylsiloxy-1-ethoxyethene and silyl nucleophiles (triethylsilane, allyltrimethylsilane, trimethylsilyl cyanide, etc.) in the pr
- Mukaiyama, Teruaki,Homma, Koichi,Takenoshita, Haruhiro
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p. 1725 - 1728
(2007/10/02)
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