147754-12-9Relevant articles and documents
Practical CuCl/DABCO/4-HO-TEMPO-catalyzed oxidative synthesis of nitriles from alcohols with air as oxidant
Hu, Yongke,Chen, Lei,Li, Bindong
supporting information, p. 464 - 466 (2017/11/13)
A mild and efficient methodology for the direct oxidative synthesis of nitriles from easily available alcohols and aqueous ammonia by employing CuCl/DABCO/4-HO-TEMPO as the catalysts is described. This protocol uses the air as a green oxidant and aqueous ammonia as the nitrogen source at room temperature. A variety of aryl, heterocyclic and allylic alcohols are smoothly converted into the corresponding nitriles in good to excellent yields.
New trelagliptin preparation process
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Paragraph 0033; 0034; 0035, (2016/10/17)
The present invention provides a trelagliptin preparation process, which comprises that: 1) a compound 4 and a compound 5 are adopted as raw materials, and are subjected to a condensation reaction in an organic solvent in the presence of an alkali to obtain a compound 6; 2) the compound 6 reacts with an acid HA in an organic solvent to remove the t-butyloxy carbonyl so as to obtain a trelagliptin.HA salt; and 3) the trelagliptin.HA salt is subjected to alkali neutralization treatment and purification to obtain the trelagliptin, wherein the reaction route is defined in the specification. According to the present invention, in the improved preparation process, the 2-site amino of the compound 5 is protected by the t-butyloxy carbonyl, such that the selectivity of the nucleophilic substitution reaction is improved, and the impurity production caused by primary amine substitution is avoided so as to improve the nucleophilic substitution yield and improve the trelagliptin purity.
Cobalt-Catalyzed Electrophilic Cyanation of Arylzinc Halides with N-Cyano-N-phenyl-p-methylbenzenesulfonamide (NCTS)
Cai, Yingxiao,Qian, Xin,Rrat, Alice,Auffrant, Audrey,Gosmini, Corinne
supporting information, p. 3419 - 3423 (2016/01/25)
The cobalt-catalyzed cross-coupling of organozinc bromides with N-cyano-N-phenyl-p-methylbenzenesulfonamide (NCTS) is described. The same cobalt catalyst, cobalt(II) bromide, was used for both the synthesis of the organozinc species and the cross-coupling reaction. However in this case, a catalytic amount of zinc dust is necessary in the second step to release the low-valent cobalt. Under these mild conditions, moderate to excellent yields of different benzonitriles were obtained.