- Preparation method of 2,6-dibromoaniline
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The invention discloses a preparation method of 2,6-dibromoaniline. According to the method, 2,6-difluorobenzonitrile is used as an initial raw material, and the 2,6-dibromoaniline is synthesized through six steps of reactions including ammonolysis, diazotization bromination, re-ammonolysis, re-diazotization bromination, amidation and Hofmann degradation. The 2,6-dibromoaniline obtained in the process is a brown solid, and the purity of the 2,6-dibromoaniline is 98% or above.
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- A radical cyclization cascade of 2-alkynylbenzonitriles with sodium arylsulfinates
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A convenient radical cyclization cascade procedure for the construction of sulfonated indenones from 2-alkynylbenzonitriles and sodium arylsulfinates has been explored under mild reaction conditions. The present methodology offers a low-cost and operationally straightforward approach to synthesizing various sulfonated indenones in moderate to good yields by simple use of cheap sodium persulfate as an oxidant and environmentally benign water as a co-solvent.
- Zhou, Bang,Chen, Wenqi,Yang, Yuzhong,Yang, Yuan,Deng, Guobo,Liang, Yun
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p. 7959 - 7963
(2018/11/21)
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- Process for synthesizing 2-cyanogroup 3-fluorophenylboronic acid
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The invention relates to a process for synthesizing 2-cyanogroup 3-fluorophenylboronic acid. According to the method, 3-bromofluorobenzene is used as a raw material, and takes a reaction with LDA and dimethylformamide in a tetrahydrofuran solvent to obtain 2-fluorine 6-bromobenzaldehyde; then, the 2-fluorine 6-bromobenzaldehyde and hydroxylamine hydrochloride take a reaction at 100 DEG C to obtain 2-fluorine 6-bromoxynil; finally, triisopropyl borate is added into the intermediate; n-butyllithium is dropwise added at -70 DEG C; reduced pressure distillation is performed to obtain 2-fluorine 6-bromophenylboronic acid. The process provided by the invention has the advantages that the operation is simple and convenient; the raw material can be easily obtained; the yield is high.
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Paragraph 0030
(2017/08/29)
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- Palladium catalyzed intramolecular acylcyanation of alkenes using α-iminonitriles
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Reported here is a palladium catalyzed intramolecular acylcyanation of alkenes using α-iminonitriles. Through this method, highly functionalized indanones are synthesized in moderate to high yields using Pd(PPh 3)4, without need for any additional ligands, and a common Lewis acid (ZnCl2). Additionally, the reaction tolerates substitution at various positions on the aromatic ring including electron donating and electron withdrawing groups. This journal is the Partner Organisations 2014.
- Rondla, Naveen R.,Ogilvie, Jodi M.,Pan, Zhongda,Douglas, Christopher J.
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supporting information
p. 8974 - 8977
(2014/08/05)
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- IMIDAZO-PYRIDINE DERIVATIVES AS LIGANDS FOR GABA RECEPTORS
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A class of 8-fluoro-3-phenylimidazo[1,2-a]pyridine derivatives, substituted at the meta position of the phenyl ring by an optionally substituted aryl or heteroaryl group, or by a pyrrolidinonyl group, which is directly attached or bridged by an oxygen atom or by a -NH- or -OCH2- linkage, being selective ligands for GABAA receptors, in particular having high affinity for the α2 and/or α3 and/or α5 subunit thereof, are accordingly of benefit in the treatment and/or prevention of adverse conditions of the central nervous system, including anxiety, convulsions and cognitive disorders.
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- Direct Synthesis of 2,4-Diaminoquinazolines from 2-Fluorobenzonitriles
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In a search for new methods for preparing 2,4-diaminoquinazolines having a diversity of substituents in the benzenoid ring, it was found that the reaction of 2,6-difluorbenzonitrile with guanidine carbonate gave 2,4-diamino-5-fluoroquinazoline in excellent yield.Extension of this approach to other 2-fluorobenzonitriles, some of which were elaborated for the first time, showed that this reaction possesses considerable generality.The cyclization was sucessful even when electron donating groups were present at position six.Only in two cases where a primary or secondary amino group was also present ortho to the cyano group was this transformation unsucessful.
- Hynes, John B.,Pathak, Alpana,Panos, Constantina H.,Okeke, Claudia C.
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p. 1173 - 1177
(2007/10/02)
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