26453-01-0Relevant articles and documents
Nickel-Catalyzed Cyanation of Unactivated Alkyl Sulfonates with Zn(CN)2
Xia, Aiyou,Lv, Peizhuo,Xie, Xin,Liu, Yuanhong
supporting information, p. 7842 - 7847 (2020/11/02)
Cyanation of unactivated primary and secondary alkyl mesylates with Zn(CN)2 catalyzed by nickel has been developed. The reaction provides an efficient route for the synthesis of alkyl nitriles with wide substrate scope, good functional group tolerance, and compatibility with heterocyclic compounds. Mechanistic studies indicate that alkyl iodide generated in situ serves as the reactive intermediate and the gradual release of alkyl iodide is crucial for the success of the reaction.
Preparation method of alkyl nitrile compound
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Paragraph 0189-0191; 0198-0200, (2020/05/14)
The invention discloses a preparation method of an alkyl nitrile compound shown as formula I. The preparation method comprises the following step: in a solvent, in the presence of an additive and a catalyst, Zn (CN) 2 and an alkyl halide shown as formula II are subjected to a coupling reaction as shown in the specification to obtain the alkyl nitrile compound as shown in the formula I, wherein theadditive comprises an alkali, the catalyst comprises a nickel compound and a phosphine ligand; the nickel compound is one or more of zero-valent nickel, monovalent nickel salt and divalent nickel salt; when the nickel compound contains zero-valent nickel or divalent nickel salt, the catalyst further comprises a reducing agent. According to the preparation method disclosed by the invention, cyanation of an alkyl halide can be simply, conveniently and efficiently realized by using a cheap catalytic system, and the preparation method also has good functional group compatibility and substrate universality.
Novel method for synthesizing 2-amine indene
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Paragraph 0049; 0050-0051; 0056-0058; 0063-0065, (2019/03/31)
The invention provides a novel method for synthesizing 2-amine indene. The novel method includes carrying out nucleophilic substitution reaction on bisbenzene and ethyl cyanoacetate and carrying out decarboxylation procedures to obtain compounds 15; carrying out hydrolysis to obtain compounds 16; ultimately carrying out Hofmann degradation reaction to obtain the 2-amine indene which is a target product. The bisbenzene is a chemical material and is used as a main raw material for the 2-amine indene. Compared with the prior art, the novel method has the advantages that the novel method is shortin reaction path and suitable for industrial large-scale production, raw materials are low in cost and are easily available, reaction conditions are mild, the productivity can be obviously improved, and the production cycle can be obviously shortened.
Nickel-Catalyzed Cyanation of Unactivated Alkyl Chlorides or Bromides with Zn(CN)2
Xia, Aiyou,Xie, Xin,Chen, Haoyi,Zhao, Jidong,Zhang, Chunli,Liu, Yuanhong
supporting information, p. 7735 - 7739 (2019/01/03)
A nickel-catalyzed cyanation of unactivated secondary alkyl chlorides or bromides using less toxic Zn(CN)2 as the cyanide source has been developed. The reaction features the use of air-stable and inexpensive NiCl2·6H2O or Ni(acac)2 as the precatalysts and offers an efficient synthesis of a broad range of alkyl nitriles. Cyanation of primary alkyl chlorides or bromides was also achieved by reaction with Zn(CN)2 in the presence of n-Bu4NCl without the need of nickel catalyst.
AMINOMETHYL SUBSTITUTED BICYCLIC AROMATIC COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO MODULATION OF THE DOPAMINE D3 RECEPTOR
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Page/Page column 106, (2010/11/08)
The present invention relates to an aminomethyl substituted bicyclic aromatic compound of the formula (I) wherein Ar is a cyclic radical selected from the group consisting of phenyl, a 5- or 6-membered C-bound heteroaromatic radical comprising as ring mem
Diaminoindanes as microsomal triglyceride transfer protein inhibitors
Ksander,DeJesus,Yuan,Fink,Moskal,Carlson,Kukkola,Bilci,Wallace,Neubert,Feldman,Mogelesky,Poirier,Jeune,Steele,Wasvery,Stephan,Cahill,Webb,Navarrete,Lee,Gibson,Alexander,Sharif,Hospattankar
, p. 4677 - 4687 (2007/10/03)
The synthesis and biological activities of biarylamide-substituted diaminoindanes as microsomal triglyceride transfer protein (MTP) inhibitors are described. One of the more potent compounds, 8aR, inhibited both the secretion of apoB from Hep G2 cells and the MTP-mediated transfer of triglycerides between synthetic acceptor and donor liposomes with IC50 values of 0.7 and 70 nM, respectively. In normolipidemic rats and dogs, oral administration of 8aR dose-dependently reduced both plasma triglycerides and total cholesterol. Moreover, in rats and dogs, 8aR also prevented the postprandial rise in plasma triglycerides following a bolus administration of a fat load. Because MTP inhibitors decrease very low density lipoprotein assembly in the liver, the potential for hepatic lipid accumulation was evaluated. In normolipidemic rats, hepatic cholesterol and triglyceride contents were dose-dependently increased by 8aR. However, hepatic lipid accumulation resulted in negligible change in total liver weight and was reversible after withdrawal of the compound.