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Rhodium-Catalyzed Addition of Organozinc Iodides to Carbon-11 Isocyanates
Fouad, Moustafa H.,Ismailani, Uzair S.,Mair, Braeden A.,Munch, Maxime,Rotstein, Benjamin H.
, p. 2746 - 2750 (2020/04/16)
Amides were prepared using rhodium-catalyzed coupling of organozinc iodides and carbon-11 (11C, t1/2 = 20.4 min) isocyanates. Nonradioactive isocyanates and sp3 or sp2 organozinc iodides generated amides in yields of 13%-87%. Incorporation of cyclotron-produced [11C]CO2 into 11C-amide products proceeded in yields of 5%-99%. The synthetic utility of the methodology was demonstrated through the isolation of [11C]N-(4-fluorophenyl)-4-methoxybenzamide ([11C]6g) with a molar activity of 267 GBq μmol-1 and 12% radiochemical yield in 21 min from the beginning of synthesis.
Transition-metal-free mono- or dinitration of protected anilines
Dai, Enrui,Dong, Ying,Dong, Yongrui,Kong, Rui,Liang, Deqiang,Liu, Guangzhang,Ma, Yinhai,Wu, Qiong
, (2020/04/27)
An amide-assisted arene nitration is presented, and both mono- and dinitration of protected anilines could be effected by using NaNO2 and NaNO3 as the mono- and bisnitrating agents, respectively. This divergent synthesis is transition-metal- and acid-free, and features a broad substrate scope, low cost, and ortho–para selectivity.
A kind of sphingomyelin synthase inhibitor, its preparation method and application thereof
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Paragraph 0203; 0204; 0205; 0206, (2019/07/11)
The invention provides general formula (I) compound of formula, its pharmaceutically acceptable salts or stereoisomers, wherein X, Y, M, Z, R and Ar respectively as defined in the specification. The invention also provides a composition comprising a therapeutically effective amount of at least one of the foregoing general formula (I) compounds of formula, its pharmaceutically acceptable salts or stereoisomers, and the above-mentioned compound, its pharmaceutically acceptable salts or stereoisomers, or the above-mentioned pharmaceutical composition in preparation for the prevention and/or treatment of sphingomyelin level abnormal increase of the disease caused by the use of the medicament. The invention of the general formula (I) compound of formula, its pharmaceutically acceptable salts or stereoisomers, can selectively inhibit sphingomyelin synthase, internal and external pharmacodynamic effects are significant, the safety is high.