267651-23-0Relevant articles and documents
Redox-Neutral Coupling between Two C(sp3)?H Bonds Enabled by 1,4-Palladium Shift for the Synthesis of Fused Heterocycles
Rocaboy, Ronan,Anastasiou, Ioannis,Baudoin, Olivier
supporting information, p. 14625 - 14628 (2019/09/16)
The intramolecular coupling of two C(sp3)?H bonds to forge a C(sp3)?C(sp3) bond is enabled by 1,4-Pd shift from a trisubstituted aryl bromide. Contrary to most C(sp3)?C(sp3) cross-dehydrogenative couplings, this reaction operates under redox-neutral conditions, with the C?Br bond acting as an internal oxidant. Furthermore, it allows the coupling between two moderately acidic primary or secondary C?H bonds, which are adjacent to an oxygen or nitrogen atom on one side, and benzylic or adjacent to a carbonyl group on the other side. A variety of valuable fused heterocycles were obtained from easily accessible ortho-bromophenol and aniline precursors. The second C?H bond cleavage was successfully replaced with carbonyl insertion to generate other types of C(sp3)-C(sp3) bonds.
Preparation method for intermediates of new medicine Lusutrombopag resisting to thrombopenia
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, (2017/08/15)
The invention discloses a preparation method for intermediates of a new medicine Lusutrombopag resisting to thrombopenia. According to the invention, column chromatography of each step is avoided through an effective method with regard to preparation for an intermediate I, and in addition, bromo-compounds are used for replacing chloro-compounds in the step of ring closure, thus the ring closure has a quantitative yield and is quite easy to operate. In addition, the second carbonyl group and bromine are introduced stepwise, thus the two steps achieve a yield of more than 80%, and are stable and easy to repeat. Compared with the yield of 25-30% of the last two steps of the original research document, the yield is greatly increased, and the preparation method is simple and convenient to operate, and easy to repeat. According to the invention, synthesis for an intermediate II is realized with a quite high yield (70-80%) and an extremely short route through two effective strategies with regard to the intermediate II.
CARBAZOLE COMPOUNDS AND METHODS OF USING SAME
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Paragraph 00120, (2015/02/25)
The present invention provides carbazole compounds of the formula (I), which can be used for treating microbial, protozoan, viral infections and cancer. ?