- Aminoazanium of DABCO: An Amination Reagent for Alkyl and Aryl Pinacol Boronates
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The aminoazanium of DABCO (H2N-DABCO) has been developed as a general and practical amination reagent for the direct amination of alkyl and aryl pinacol boronates. This compound is stable and practical for use as a reagent. Various primary, secondary. and tertiary alkyl?Bpin and aryl?Bpin substrates were aminated to give the corresponding amine derivatives. The amination is stereospecific. The anti-Markovnikov hydroamination of olefins was easily achieved by catalytic hydroboration with HBpin and in subsequent situ amination using H2N-DABCO. Moreover, the combination of 1,2-diboration of olefins, using B2pin2, with this amination process achieved the unprecedented 1,2-diamination of olefins. The amination protocol was also successfully extended to aryl pinacol boronates.
- Liu, Xingxing,Zhu, Qing,Chen, Du,Wang, Lu,Jin, Liqun,Liu, Chao
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supporting information
p. 2745 - 2749
(2020/01/25)
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- Amination reagent as well as preparation method and application thereof
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The invention discloses an amination reagent as well as a preparation method and application thereof. The amination reagent has a structure as shown in a formula disclosed in the invention, wherein Xis selected from any one of I, Cl, Br, NO3 and ClO4, and Y and Z are independently selected from H or alkyl with the carbon atom number of 1-4. The process for preparing the amination reagent is simple, the raw materials are easy to obtain, the cost is low, the yield is stable, and the prepared amination reagent is stable in character, can be stored at room temperature for a long time and can be taken as needed; meanwhile, the prepared amination reagent is efficient in performance, boron substrate applicability is excellent, reaction effect is good, and limitation of amination reaction of organic boron compounds on substrates is greatly expanded.
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Paragraph 0142-0144; 0148-0149; 0174
(2020/03/12)
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- Catalytic reduction of amides to amines by electrophilic phosphonium cations via FLP hydrosilylation
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A catalytic methodology for the conversion of amides to amines is reported. Of the 25 examples described, 14 examples involve the reduction of N-trifluoroacetamides to the corresponding trifluoroethylamines. These reductions are achieved by catalytic hydrosilylation of the amide mediated by an electrophilic phosphonium cation (EPC) catalyst.
- Augurusa, Alessandra,Mehta, Meera,Perez, Manuel,Zhu, Jiangtao,Stephan, Douglas W.
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supporting information
p. 12195 - 12198
(2016/10/21)
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- COMPOSITIONS AND METHODS FOR INHIBITION OF THE JAK PATHWAY
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Disclosed are compounds of formula I, compositions containing them, and methods of use for the compounds and compositions in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK 2 and JAK3, are
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Page/Page column 60
(2012/02/06)
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- PIPERAZINE DERIVATIVES USEFUL AS CCR5 ANTAGONISTS
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The use is described of CCR5 antagonists of formula (I) or a pharmaceutically acceptable salt thereof, wherein: R is optionally substituted phenyl, pyridyl, thiophenyl or naphthyl; R 1 is hydrogen or alkyl; R 2 is substituted phenyl, substituted heteroary
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Page/Page column 29
(2010/02/12)
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