117-47-5Relevant articles and documents
Regiospecific S-aminoalkylation of 5-substituted 6-hydroxy-2-thiouracil derivatives in the synthesis of structural analogs of isothiobarbamine
Brunilina, L. L.,Chapurkin, V. V.,Deshevov, P. P.,Kirillov, I. A.,Korenkov, B. D.,Nawrozkij, M. B.,Novakov, I. A.,Sheikin, D. S.,Vostrikova, O. V.
, p. 943 - 948 (2021)
Regiospecific S-monoaminoalkylation of 5-substituted derivatives of 6-hydroxy-2-thiouracil with free N,N-dialkyl-N-(2-chloroethyl)amines in anhydrous PriOH was described for the first time. In compliance with the rules and regulations of green chemistry, this approach was used to synthesize a number of structural analogs of isothiobarbamine in high yield and purity, which are potential synthetic actoprotectors of immediate action.
Dehydroxymethylation of alcohols enabled by cerium photocatalysis
Zhang, Kaining,Chang, Liang,An, Qing,Wang, Xin,Zuo, Zhiwei
supporting information, p. 10556 - 10564 (2019/08/20)
Dehydroxymethylation, the direct conversion of alcohol feedstocks as alkyl synthons containing one less carbon atom, is an unconventional and underexplored strategy to exploit the ubiquity and robustness of alcohol materials. Under mild and redox-neutral reaction conditions, utilizing inexpensive cerium catalyst, the photocatalytic dehydroxymethylation platform has been furnished. Enabled by ligand-to-metal charge transfer catalysis, an alcohol functionality has been reliably transferred into nucleophilic radicals with the loss of one molecule of formaldehyde. Intriguingly, we found that the dehydroxymethylation process can be significantly promoted by the cerium catalyst, and the stabilization effect of the fragmented radicals also plays a significant role. This operationally simple protocol has enabled the direct utilization of primary alcohols as unconventional alkyl nucleophiles for radical-mediated 1,4-conjugate additions with Michael acceptors. A broad range of alcohols, from simple ethanol to complex nucleosides and steroids, have been successfully applied to this fragment coupling transformation. Furthermore, the modularity of this catalytic system has been demonstrated in diversified radical-mediated transformations including hydrogenation, amination, alkenylation, and oxidation.
Secobarbital artificial antigen and preparation method thereof
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Paragraph 0029; 0058-0062, (2018/09/28)
The objective of the invention is to provide a secobarbital artificial antigen and a preparation method thereof. According to the invention, malonate and urea are used as main raw materials for synthesis of the secobarbital antigen. The method comprises the following steps: reacting halogenated pentane with malonate to prepare 2-(1-methylbutyl)malonate; subjecting a malonate derivative and urea toa cyclization reaction to prepare barbitone derivative; reacting long-chain halogenated olefine acid with the barbitone derivative to prepare a hapten; and reacting the hapten reacts with N-hydroxysuccinimide and N,N-cyclohexylcarbodiimide under nitrogen protection to obtain active ester, subjecting the active ester and a protein to a coupling reaction, and simultaneously removing a trifluoroacetyl protecting group so as to obtain the secobarbital artificial antigen. The preparation method provided by the invention is simple in process, low in production cost, and not limited in raw materialsources. The prepared artificial antigen can be used for animal immunization to obtain corresponding antibodies, is used for the research of various barbitone immunoassays and the production of rapiddetection kits, and has a wide application scope.
