- Scalable and Straightforward Synthesis of All Isomeric (Cyclo)alkylpiperidines
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An efficient approach towards introducing (cyclo)alkyl substituents at C-2, C-3 or C-4 positions of the piperidine ring was described. The method relied on the straightforward two-step reaction sequence based on the formal sp3–sp3 re
- Subota, Andrii I.,Lutsenko, Anton O.,Vashchenko, Bohdan V.,Volochnyuk, Dmitriy M.,Levchenko, Vitalina,Dmytriv, Yurii V.,Rusanov, Eduard B.,Gorlova, Alina O.,Ryabukhin, Sergey V.,Grygorenko, Oleksandr O.
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p. 3636 - 3648
(2019/06/13)
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- A new strategy for deprotonative functionalization of aromatics: Transformations with excellent chemoselectivity and unique regioselectivities using t-Bu-P4 base
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A new strategy for deprotonative functionalization of aromatics using t-Bu-P4 base has been developed, and highly chemoselective transformations have been achieved with unique regioselectivities. Copyright
- Imahori, Tatsushi,Kondo, Yoshinori
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p. 8082 - 8083
(2007/10/03)
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- New syntheses of substituted pyridines via bromine-magnesium exchange
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Bromine-magnesium exchange using iPrMgCl in THF at room temperature on 2-, 3- and 4-bromopyridines allowed the synthesis of various functionalized pyridines. The methodology was successfully used for the synthesis of 4- azaxanthone. Moreover, single exchange reactions observed on 2,6-, 3,5-, 2,3- and 2,5-dibromopyridines, with complete regioselectivity in the case of 2,3- and 2,5-dibromopyridines, afforded substituted bromopyridines, which were then involved in a second exchange step to provide difunctionalized pyridines. (C) 2000 Elsevier Science Ltd.
- Trécourt, Fran?ois,Breton, Gilles,Bonnet, Véronique,Mongin, Florence,Marsais, Francis,Quéguiner, Guy
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p. 1349 - 1360
(2007/10/03)
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- Pyridylmagnesium chlorides from bromo and dibromopyridines by bromine- magnesium exchange: A convenient access to functionalized pyridines
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Various bromopyridines were converted to the corresponding pyridylmagnesium chlorides at room temperature by treatment with iPrMgCl. The resulting Grignard reagents were quenched by various electrophiles to afford functionalized pyridines. The bromine-magnesium exchange of some dibromopyridines was also studied.
- Trecourt, Francois,Breton, Gilles,Bonnet, Veronique,Mongin, Florence,Marsais, Francis,Queguiner, Guy
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p. 4339 - 4342
(2007/10/03)
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- Potent inhibitors of protein farnesyltransferase: Heteroarenes as cysteine replacements
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Synthesis and biological evaluation of heteroarenes as reduced cysteine replacements are described. Of the heteroaryl groups examined with respect to FT inhibitor FTI-276 (1), pyridyl was the replacement found to be most effective. Substitutions at C4 of the pyridyl moiety did not affect the in vitro activity. Compound 9a was found to have moderate in vivo bioavailability.
- Shen, Wang,Fakhoury, Stephen,Donner, Greg,Henry, Kenneth,Lee, Jang,Zhang, Haichao,Cohen, Jerry,Warner, Robert,Saeed, Badr,Cherian, Sajeev,Tahir, Stephen,Kovar, Peter,Bauch, Joy,Ng, Shi-Chung,Marsh, Kennan,Sham, Hing,Rosenberg, Saul
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p. 703 - 708
(2007/10/03)
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- A NEW SOURCE FOR GENERATION OF BENZYNE AND PYRIDYNE: REACTIONS OF O-HALOPHENYL (OR 3-BROMO-4-PYRIDYL) PHENYL SULFOXIDES WITH GRIGNARD REAGENTS
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o-Chloro- and o-bromophenyl phenyl sulfoxides and (3-bromo-4-pyridyl) phenyl sulfoxide were treated with Grignard reagents to generate benzyne (or 3,4-pyridyne) in THF.The o-iodophenyl derivative, on the other hand, gave mainly o-(arylsulfinyl)phenyl Grignard reagent.
- Furukawa, Naomichi,Shibutani, Tadao,Fujihara, Hisashi
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p. 2727 - 2730
(2007/10/02)
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