- Arylation, Vinylation, and Alkynylation of Electron-Deficient (Hetero)arenes Using Iodonium Salts
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Arylation, vinylation, and alkynylation of electron-deficient arenes and heteroarenes have been achieved by chemoselective C-H zincation followed by copper-catalyzed coupling reactions using iodonium salts. This approach offers a direct and general access to a wide scope of (hetero)biaryls as well as alkenylated and alkynylated heteroarenes under mild conditions. It is particularly useful and valuable for the rapid and modular synthesis of diverse (hetero)aryl compounds, as demonstrated in the synthesis of transient receptor potential vanilloid 1 (TRPV1) antagonists and angiotensin II receptor type 1 (AT1 receptor) antagonists.
- Liu, Chuan,Wang, Qiu
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supporting information
p. 5118 - 5121
(2016/10/14)
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- NEW SUBSTITUTED BIPHENYL ANALOGUES AS DUAL INHIBITORS OF AROMATASE AND SULFATASE
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Provided are new biphenyl derivatives of formula (Ia). These compounds act as aromatase and sulfatase inhibitors. They are particularly useful for treating pathological conditions or diseases in which aromatase and sulfatase are involved. Moreover, provided are processes for the preparation of these compounds and pharmaceutical compositions containing said products and their use for the preparation of a medicament, in particular for the treatment of diseases characterized by aromatase and sulfatase activity such as hormone-dependent cancers.
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Page/Page column 44
(2015/07/16)
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- Cross-coupling study of iodo/chloropyridines and 2-chloroquinoline with atom-economic triarylbismuth reagents under Pd-catalysis
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This study describes the palladium-catalyzed couplings of iodopyridines, chloropyridines, and chloroquinoline with atom-economic BiAr3 reagents in sub-stoichiometric loadings. Mono-arylations of iodo and chloropyridines produced arylpyridines i
- Rao, Maddali L.N.,Dhanorkar, Ritesh J.
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p. 338 - 349
(2015/03/04)
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- Triarylbismuthanes as threefold aryl-transfer reagents in regioselective cross-coupling reactions with bromopyridines and quinolines
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Cross-coupling studies using bromopyridines and bromoquinolines with triarylbismuths as threefold coupling reagents in substoichiometric amounts under Pd-catalysed conditions are disclosed. The reactivity was high with both mono- and dibromopyridyl substrates, and mono- and bis-couplings were carried out regioselectively. A library of monoaryl and diaryl pyridines was formed in high yields. A one-pot strategy provided a simple and straightforward synthesis of both symmetrical and unsymmetrical diarylpyridines. Arylations of 2-bromo- and 3-bromoquinolines were achieved with triarylbismuth reagents. This study demonstrates that triarylbismuths may be used as threefold arylating reagents for the synthesis of aryl pyridines and quinolines through couplings with bromopyridines and bromoquinolines under Pd-catalysed conditions. Copyright
- Rao, Maddali L.N.,Dhanorkar, Ritesh J.
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supporting information
p. 5214 - 5228
(2014/10/15)
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- Practical one-pot preparation of magnesium Di(hetero)aryl- and magnesium dialkenylboronates for Suzuki-Miyaura cross-coupling reactions
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Mg for B: An atom-economical one-pot synthesis by direct magnesium insertion in the presence of B(OBu)3 and LiCl allows a broad range of functionalized (hetero)aryl and alkenyl bromides to be converted into magnesium diorganoboronates 2, which
- Haag, Benjamin A.,Saemann, Christoph,Jana, Anukul,Knochel, Paul
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supporting information; experimental part
p. 7290 - 7294
(2011/09/16)
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- Highly selective metalations of pyridines and related heterocycles using new frustrated lewis pairs or tmp-zinc and tmp-magnesium bases with bf 3·oet2
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(Figure Presented) Efficient and selective: Frustrated Lewis pairs based on BF3·OEt2 and LiCl-com-plexed tmpMg or tmpZn amides (tmp = 2,2,6,6-tetramethylpiperidyl) allow the efficient and regioselective metalation of various functionalized N heterocycles (see scheme for examples). Moreover, such metalations carried out in the presence or absence of BF 3·OEt2 enable a complete switch of regioselectivity, thus allowing complementary fuctionalization.
- Jaric, Milica,Haag, Benjamin A.,Unsinn, Andreas,Karaghiosoff, Konstantin,Knochel, Paul
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supporting information; experimental part
p. 5451 - 5455
(2010/09/16)
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