- Visible-light-promoted aerobic metal-free aminothiocyanation of activated ketones
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A direct, redox-neutral, highly atom-economical and metal-free aerobic method for the synthesis of multi-substituted olefins via simply coupling ammonium thiocyanate with activated ketones is described. A series of multi-substituted olefins could be easil
- Yuan, Pan-Feng,Zhang, Qing-Bao,Jin, Xiao-Ling,Lei, Wen-Long,Wu, Li-Zhu,Liu, Qiang
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Read Online
- Convenient and simple synthesis of 2-aminothiazoles by the reaction of α-halo ketone carbonyls with ammonium thiocyanate in the presence of N-methylimidazole
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Substituted 2-aminothiazole derivatives were obtained as a result of N-methylimidazole catalyzed cyclization of α-halo ketone carbonyls with ammonium thiocyanate in water-alcoholic media. The generality of the method has been demonstrated by screening a series of aromatic/heteroaromatic/aliphatic α-halo ketones, α-halo β-diketones, and α-halo β-ketoesters. The developed method is simple, mild, and general route for the preparation of diversely functionalized 2-aminothiazoles in good to moderate yields from readily available starting materials.
- Meshram,Thakur, Pramod B.,Madhu Babu,Bangade, Vikas M.
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p. 5265 - 5269
(2012/10/30)
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- I2/CuO-catalyzed tandem cyclization strategy for one-pot synthesis of substituted 2-aminothiozole from easily available aromatic ketones/α,β-unsaturated ketones and thiourea
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A concise and efficient one-pot process from easily available methyl ketones/unsaturated methyl ketones and thiourea was developed for the synthesis of 2-aminothiazoles under the media of I2/CuO. The method can highly stereoselectivity obtain the E-isomers of 4-ethenyl-2-aminothiazoles (5a-f). All these target molecules were characterized by NMR, HRMS and IR spectra. Furthermore, the target compounds 3c and 5b were further determined by X-ray crystallographic analysis.
- Zhu, Yan-Ping,Yuan, Jing-Jing,Zhao, Qin,Lian, Mi,Gao, Qing-He,Liu, Mei-Cai,Yang, Yan,Wu, An-Xin
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supporting information; experimental part
p. 173 - 178
(2012/01/05)
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- Xanthan sulfuric acid: An efficient bio-supported and recyclable solid acid catalyst for the synthesis of 2-aminothiazole-5-carboxylates and 2-aminoselenazole-5-carboxylates
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An efficient method has been developed for the synthesis of 2-amino thiazole and selenazole-5-carboxylates from β-ketoesters, thiourea or seleno urea and N-bromo succinamide by using Xanthan sulfuric acid as a solid acid catalyst. The reaction work-up is
- Kuarm, Bowroju S.,Madhav, Janganati V.,Rajitha, Bhargavi
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experimental part
p. 549 - 553
(2012/06/04)
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- Aqueous-phase one-pot synthesis of 2-aminothiazole- or 2-aminoselenazole-5- carboxylates from β-keto esters, thiourea or selenourea, and N-bromosuccinimide under supramolecular catalysis
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2-Amino-4-alkyl- and 2-amino-4-arylthiazole-5-carboxylates and their selenazole analogues were synthesized by α-halogenation of β-keto esters with N-bromosuccinimide, followed by cyclization with thiourea or selenourea, respectively, in the presence of β-
- Narender, Mendu,Reddy, Majjigapu Somi,Kumar, Vydyula Pavan,Srinivas, Boga,Sridhar, Regati,Nageswar, Yadavalli Venkata Durga,Rao, Kakulapati Rama
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p. 3469 - 3472
(2008/09/19)
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- 2,6-Substituted chroman derivatives useful as beta-3 adrenoreceptor agonists
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This invention relates to novel 2,6-substituted chroman derivatives which are useful in the treatment of beta-3 adrenoreceptor-mediated conditions.
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- Di-substituted aminomethyl-chroman derivative beta-3 adrenoreceptor agonists
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This invention is related to novel di-substituted aminomethyl chroman derivatives which are useful in the treatment of beta-3 receptor-mediated conditions.
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- SUBSTITUTED QUINAZOLINE DERIVATIVES AND THEIR USE AS INHIBITORS
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The use of a compound of formula (I) 1 or a salt, ester or amide thereof; where X is O, or S, S(O) or S(O)2, or NR6 where R6 is hydrogen or C1-6 alkyl,; R5 is an optionally substituted 5-membered heteroaromatic ring, R1, R2 ,R3, R4 are independently selected from various specified moieties, in the preparation of a medicament for use in the inhibition of aurora 2 kinase. Certain compounds are novel and these, together with pharmaceutical compositions containing them are also described and claimed
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- Benzofuran and dihydrobenzofuran derivatives useful as beta-3 adrenoreceptor agonists
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This invention relates to novel benzofuran and dihydrobenzofuran compounds, pharmaceutical compositions containing such compounds, and methods of treating beta-3 adrenoreceptor-mediated conditions with such compositions.
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Page/Page column 35
(2010/01/31)
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- INHIBITORS OF FACTOR XA WITH A NEUTRAL P1 SPECIFICITY GROUP
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The present application describes inhibitors of factor Xa with a neutral P1 specificity group of formula I: STR1 or pharmaceutically acceptable salt forms thereof, wherein R and E may be groups such as methoxy and halo.
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