- Chemoselective Schwartz Reagent Mediated Reduction of Isocyanates to Formamides
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Addition of the in situ generated Schwartz reagent to widely available isocyanates constitutes a chemoselective, high-yielding, and versatile approach to the synthesis of variously functionalized formamides. Steric and electronic factors or the presence of sensitive functionalities (esters, nitro groups, nitriles, alkenes) do not compromise the potential of the method. Full preservation of the stereochemical information contained in the starting materials is observed. The use of formamides in the nucleophilic addition of organometallic reagents (Chida-Sato allylation, Charette-Huang addition to imidoyl triflate activated amides, Matteson homologation of boronic esters) is briefly investigated.
- Pace, Vittorio,De La Vega-Hernández, Karen,Urban, Ernst,Langer, Thierry
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supporting information
p. 2750 - 2753
(2016/06/15)
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- HETEROARYL COMPOUNDS, SYNTHESIS THEREOF, AND INTERMEDIATES THERETO
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The present invention relates to methods for synthesizing compounds useful as inhibitors or both of ERK1 and ERK2 kinase, derivatives thereof, and intermediates thereto.
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Paragraph 00386-00388
(2016/12/07)
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- 4,5,6,7-tetrahydrobenzimidazole derivatives as 5HT3 -antagonists
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4,5,6,7-Tetrahydrobenzimidazole derivatives represented by general formula (I) STR1 wherein groups represents the following: R1, R2, R3 : independently represent hydrogen atom, hydroxy group, a halogen atom, a lower alkyl
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- o-Nitroaniline Derivatives. Part 9. Benzimidazole N-Oxides Unsubstituted at N-1 and C-2
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Since previous routes to the title compounds (1) have proved unsatisfactory as general methods, a simple new synthesis has been devised.N-Cyanomethyl-o-nitroanilines (5) are cyclised in basic media, giving 2-cyanobenzimidazole N-oxides (12) in good yield.Hydrolysis of these products with hydrochloric acid gives, directly, the title compounds as their hydrochloride salts (13), which may be isolated and purified, and which give the free N-oxides (1) by treatment with aqueous ammonia followed by evaporation. o-Nitrophenylglycine esters (4) may satisfactorily replace the nitriles (5) in certain cases.A modification of this kind in the related nitropyridylglycine series leads to 3H-imidazolpyridine 1-oxide (20).
- Harvey, Ian W.,McFarlane, Michael D.,Moody, David J.,Smith, David M.
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p. 681 - 690
(2007/10/02)
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