- Practical and regioselective amination of arenes using alkyl amines
-
The formation of carbon–nitrogen bonds for the preparation of aromatic amines is among the top five reactions carried out globally for the production of high-value materials, ranging from from bulk chemicals to pharmaceuticals and polymers. As a result of this ubiquity and diversity, methods for their preparation impact the full spectrum of chemical syntheses in academia and industry. In general, these molecules are assembled through the stepwise introduction of a reactivity handle in place of an aromatic C–H bond (that is, a nitro group, halogen or boronic acid) and a subsequent functionalization or cross-coupling. Here we show that aromatic amines can be constructed by direct reaction of arenes and alkyl amines using photocatalysis, without the need for pre-functionalization. The process enables the easy preparation of advanced building blocks, tolerates a broad range of functionalities, and multigram scale can be achieved via a batch-to-flow protocol. The merit of this strategy as a late-stage functionalization platform has been demonstrated by the modification of several drugs, agrochemicals, peptides, chiral catalysts, polymers and organometallic complexes.
- Ruffoni, Alessandro,Juliá, Fabio,Svejstrup, Thomas D.,McMillan, Alastair J.,Douglas, James J.,Leonori, Daniele
-
p. 426 - 433
(2019/05/01)
-
- Method for preparing Delmanid high-purity intermediate by one-pot method
-
The invention relates to a method for preparing a Delmanid high-purity intermediate by a one-pot method, and belongs to the technical field of chemical medicines. The preparation method comprises thefollowing steps: (1) carrying out a Buchwald-Hartwig ary
- -
-
-
- EPOXY COMPOUND AND METHOD FOR MANUFACTURING THE SAME
-
The present invention provides a novel intermediate for manufacturing a 2,3-dihydroimidazo[2,1-b]oxazole compound with a high yield and a high purity, and a manufacturing method of the intermediate. The present invention provides an epoxy compound represe
- -
-
Page/Page column 42-43
(2009/01/20)
-
- Synthesis and antituberculosis activity of a novel series of optically active 6-nitro-2,3-dihydroimidazo[2,1-b]oxazoles
-
In an effort to develop potent new antituberculosis agents that would be effective against both drug-susceptible and drug-resistant strains of Mycobacterium tuberculosis, we prepared a novel series of optically active 6-nitro-2,3-dihydroimidazo[2,1-b]oxaz
- Sasaki, Hirofumi,Haraguchi, Yoshikazu,Itotani, Motohiro,Kuroda, Hideaki,Hashizume, Hiroyuki,Tomishige, Tatsuo,Kawasaki, Masanori,Matsumoto, Makoto,Komatsu, Makoto,Tsubouchi, Hidetsugu
-
p. 7854 - 7860
(2007/10/03)
-
- METHOD OF PRODUCING AMINOPHENOL COMPOUNDS
-
The present invention provides an industrially advantageous method of producing aminophenol compounds represented by the formula (1) by a simple and easy procedure at a high yield and a high purity. The present invention provides a method of producing an aminophenol compound represented by the formula (1): (wherein each of R1 and R2, which may be the same or different, is a hydrogen atom, a substituted or unsubstituted lower alkyl group or the like; R1 and R2, taken together with the adjacent nitrogen atom, may form a 5- or 6-membered heterocycle with or without other intervening heteroatoms; the heterocycle may be substituted by 1 to 3 substituents selected from the group consisting of a hydroxyl group, a substituted or unsubstituted lower alkyl group, a substituted or unsubstituted aryl group, a substituted or unsubstituted aryloxy group and the like; and the hydroxyl group in the formula (1) is substituted on the 2- or 4-position to the amino group on the phenyl ring), which comprises allowing a cyclohexanedione compound represented by the formula (2) to react with an amine compound represented by the formula (3) (wherein R1 and R2 are as defined above), under a neutral or basic condition.
- -
-
Page/Page column 48-49
(2010/02/14)
-