- Palladium-Catalyzed Intermolecular Oxidative Diazidation of Alkenes
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A palladium-catalyzed oxidative vicinal diazidation of alkenes has been developed, in which TMSN3 was used as azide source. Both styrenes and unactivated alkenes are suitable for this reaction. And trans-alkyldiazides were obtained as major products from cyclic alkenes with moderate to good diastereoselectivities. This reaction afforded an efficient way for the synthesis of useful 1,2-diamines after hydrogenation.
- Peng, Haihui,Yuan, Zheliang,Chen, Pinhong,Liu, Guosheng
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supporting information
p. 876 - 880
(2017/06/27)
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- Three-Component Azidation of Styrene-Type Double Bonds: Light-Switchable Behavior of a Copper Photoredox Catalyst
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[Cu(dap)2]Cl effectively catalyzes azide addition from the Zhdankin reagent to styrene-type double bonds, and subsequent addition of a third component to the benzylic position. In the presence of light, a photoredox cycle is implicated with pol
- Fumagalli, Gabriele,Rabet, Pauline T. G.,Boyd, Scott,Greaney, Michael F.
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supporting information
p. 11481 - 11484
(2015/10/14)
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- One-pot protocol to synthesize N-(β-nitro)amides by tandem Henry/Ritter reaction
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A novel, efficient and atom economical one pot protocol for the synthesis of N-(β-nitro)amides has been described by combining the Henry reaction with the Ritter reaction. The designed products could be obtained from easily available aldehydes, nitroalkan
- Ai, Wensi,Shi, Ronghua,Zhu, Liyan,Jiang, Dehong,Ma, Xiaobo,Yuan, Jilan,Wang, Zhouyu
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p. 24044 - 24048
(2015/03/30)
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- COMPOUNDS, THEIR PHARMACEUTICAL COMPOSITIONS AND THEIR USES AS IDH1 MUTANTS INHIBITORS FOR TREATING CANCERS
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Provided are compounds of formula (I), wherein X, Y, Z, W, V, R2, R3 and m are defined as in the description. Their pharmaceutical compositions and their uses as IDH1 mutants inhibitors for treating cancers are also provided
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- Iodine(III)-promoted intermolecular diamination of alkenes
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A rapid and productive vicinal diamination of alkenes takes place in the presence of a hypervalent iodine(III) reagent and bissulfonimides as nitrogen sources. A total of more than 60 examples are presented. The reaction is characterized by its robustness and its wide substrate scope: it proceeds selectively with both terminal and internal alkenes and tolerates a range of functional groups.
- Souto, Jose A.,Gonzalez, Yolanda,Iglesias, Alvaro,Zian, Debora,Lishchynskyi, Anton,Muniz, Kilian
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supporting information; experimental part
p. 1103 - 1111
(2012/07/17)
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- ORGANIC COMPOUNDS
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The present invention provides heterocyclicderivatives that modulate the activity of stearoyl-CoA desaturase. Methods of using such derivatives to modulate the activity of stearoyl-CoA desaturase and pharmaceutical compositions comprising such derivatives are also encompassed.
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Page/Page column 69-70
(2010/01/30)
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- Method of making imidazole-2-thiones
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The present invention provides a method of making an imidazole-2-thione which comprises the steps of reacting a vicinal diamine with a compound having a thiocarbonyl moiety and oxidizing the resulting reaction product to obtain said imidazole-2-thione.
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Page/Page column 5-6; 8
(2008/06/13)
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- Convenient method for one-pot preparation of 1,2-diamines from nitroolefins
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Convenient method for preparation of 1,2-diamine from the corresponding nitroolefin was established by successive reactions of Michael addition of O-ethylhydroxylamine to nitroolefin and reduction with hydrogen. The present preparative method was applicable to various nitroolefins by one-pot procedure.
- Imagawa, Kiyomi,Hata, Eiichiro,Yamada, Tohru,Mukaiyama, Teruaki
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p. 291 - 292
(2007/10/03)
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- Use of α-Bromo Oxime Ethers in the Synthesis of 1,2-Diamines
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Oxime ethers 1 react with ammonia and primary amines to give α-amino oxime ethers.The reaction of α-bromo oxime ethers with sodium azide affords α-azido oxime ethers.Hydrogenolysis of the azido compounds using 5percent palladium on calcium carbonate as catalyst yields the α-amino oxime ethers.The reaction of α-azido oxime ethers with lithium aluminum hydride gives 1,2-ethanediamine derivatives.The reaction of azido oxime ether 13 with LiAlH4, and subsequently the reaction of the resulting mixture of the diamines 14 and 15 with phosgene, preferably gives cis-4-pentyl-5-methyl-2-imidazolidone (16) indicating that the reduction of 13 proceeds in a stereoselective manner to furnish mainly the syn-1,2-ethanediamine 15. Key Words: Oxime ethers / α-Azido oxime ethers / α-Amino oxime ethers / 1,2-Ethanediamines
- Shatzmiller, Shimon,Bercovici, Sorin
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p. 1005 - 1010
(2007/10/02)
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- Benzodioxane-imidazoline compounds as antihypertensives
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Compounds of the formula STR1 and the pharmaceutically acceptable acid addition salts thereof, wherein: n is an integer equal to 0, 1, 2 or 3; R1 is hydrogen, lower alkyl, optionally substituted phenyl or optionally substituted phenyl lower alkyl; each R is independently hydrogen, lower alkyl, optionally substituted phenyl, or optionally substituted phenyl lower alkyl; are α2 blockers, and, therefore, are useful in treating essential hypertension and depression, and in inhibiting platelet aggregation.
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