- Rhodium(II)-catalyzed cross-coupling of diazo compounds
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Nothing left to chance: A convenient protocol for selective cross-coupling of diazo compounds for the convergent synthesis of alkenes was developed (see scheme; EDG=aryl, heteroaryl, vinyl; R=O-alkyl, aryl). The selectivity control elements were identifie
- Hansen, Joorn H.,Parr, Brendan T.,Pelphrey, Philip,Jin, Quihui,Autschbach, Jochen,Davies, Huw M. L.
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supporting information; experimental part
p. 2544 - 2548
(2011/04/27)
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- Quinolones as gonadotropin releasing hormone (GnRH) antagonists: Simultaneous optimization of the C(3)-aryl and C(6)-substituents
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A series of 3-arylquinolones was prepared and evaluated for their ability to act as gonadotropin releasing hormone (GnRH) antagonists. A variety of substitution patterns of the 3-aryl substituent are described. The 3,4,5-trimethylphenyl substituent (23h) was found to be optimal. (C) 2000 Elsevier Science Ltd. All rights reserved.
- Young, Jonathan R.,Huang, Song X.,Chen, Irene,Walsh, Thomas F.,DeVita, Robert J.,Wyvratt Jr., Matthew J.,Goulet, Mark T.,Ren, Ning,Lo, Jane,Yang, Yi Tien,Yudkovitz, Joel B.,Cheng, Kang,Smith, Roy G.
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p. 1723 - 1727
(2007/10/03)
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- 40. Diazoaldehyde chemistry: Part 3. Synthesis of 4-acyl-1H-1,2,3-triazole derivatives
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Ten new α -diazo-β-oxoaldehydes were condensed with aniline, ammonia, hydroxylamine, and semicarbazide to yield new 4-acyl-(1-substituted)-1H-1,2,3-triazoles in moderate-to-good yields. The method is simple and regiospecific. The latter feature makes this method superior to the widely used acylacetylene + azide approach.
- Sezer, Oezkan,Dabak, Kadir,Akar, Ahmet,Anac, Olcay
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p. 449 - 453
(2007/10/03)
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- Diazoaldehyde Chemistry. Part 1. Transdiazotization of Acylacetaldehydes in Neutral-to-Acidic Medium. A Direct Approach to the Synthesis of α-Diazo-β-oxoaldehydes
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First ever non-deformylating transdiazotization of acylacetaldehydes was achieved: the reactions of 2-azido-1-ethylpyridinium tetrafluoroborate (4) with acylacetaldehydes 3 proceeded partially without deformylation to yield 16 new α-diazo-β-oxoaldehydes 1 along with diazomethyl ketones 2, especially in the presence of NaOAc (Scheme 1, Tables 1 and 2).The product distribution was substituent-dependent and could be correlated quantitatively.This new diazotization reaction appears as an alternative, direct, and more general method for the synthesis of these diazooxoaldehydes. α-Oxocycloalkanecarbaldehydes 5 gave only traces (if any) of α-diazocycloalkanones 7, and rearrangement products 6 were isolated (Scheme 2).Mechanisms of the reactions are discussed (Schemes 4 and 5).
- Sezer, Oezkan,Anac, Olcay
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p. 2323 - 2334
(2007/10/02)
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