- HCl-mediated transamidation of unactivated formamides using aromatic amines in aqueous media
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We report transamidation protocol to synthesize a range of secondary and tertiary amides from weakly nucleophilic aromatic and hetero-aryl amines with low reactive formamide derivatives, utilizing hydrochloric acid as catalyst. This current acid mediated strategy is beneficial because it eliminates the need for a metal catalyst, promoter or additives in the reaction, simplifies isolation and purification. Notably, this approach conventionally used to synthesize molecules on gram scales with excellent yields and a high tolerance for functional groups.
- Dhawan, Sanjeev,Girase, Pankaj Sanjay,Kumar, Vishal,Karpoormath, Rajshekhar
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p. 3729 - 3739
(2021/10/14)
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- Mild and facile synthesis of formamide: Reduction and functionalization of CO2 using NaBH(OAc)3 under atmospheric pressure
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An approach for N-formylation of amines was developed using NaBH(OAc)3 as a reductant under an atmospheric pressure of CO2 at 50 °C. The corresponding formylated products of various amines, including aliphatic and aromatic amines, amines with reductive-sensitive nitro groups and alkynyl groups and benzamides were obtained in good to excellent yields, and the possible reaction mechanism was also proposed.
- Liu, Huan,Nie, Zhuang,Shao, Jiaan,Chen, Wenteng,Yu, Yongping
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supporting information
p. 3552 - 3555
(2019/07/09)
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- An efficient method for the N-formylation of amines under catalyst- and additive-free conditions
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A simple catalyst- and additive-free method for the N-formylation of amines has been developed. The advantages of this protocol include a wide range of functional group tolerance, high efficiency and a lack of required extra promoters under mild conditions. This convenient strategy will provide a facile synthesis towards N-formamide natural products and pharmaceutical derivatives. A mechanism that involves difluorocarbene is proposed for this reaction.
- Xu, Zhuo-Wei,Xu, Wen-Yi,Pei, Xiao-Jun,Tang, Fei,Feng, Yi-Si
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supporting information
p. 1254 - 1258
(2019/04/10)
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- Preparation method of 3-aminophenylacetylene
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The invention relates to the field of organic synthesis, in particular to a preparation method of 3-aminophenylacetylene. The preparation method of 3-aminophenylacetylene comprises the following steps: preparing a compound shown as formula III from a compound shown as formula I and a compound shown as formula II through a coupling reaction; preparing a compound shown as formula V from the compoundshown as the formula III. The preparation method of 3-aminophenylacetylene is short in synthetic route, low in energy consumption and environmentally friendly, and the target product can be obtainedparticularly from 3-bromophenylacetylene as a raw material through two steps of reactions. Besides, prepared 3-aminophenylacetylene is used as a raw material of an anticancer drug, so that generationof potential genotoxic impurities containing halogen and ethylenic linkage structures can be avoided effectively from the source.
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Paragraph 0119-0121
(2018/09/13)
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- Facile synthesis of functionalized bis(arylethynyl)benzene derivatives via sila-Sonogashira reaction
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This article describes a facile synthesis of a new series of symmetrical bis(arylethynyl) benzene derivatives via a one-pot coupling reaction between trialkylsilyl protected arylalkynyes and aryldihalides bearing both electron-withdrawing (EW) and electrondonating groups (ED) in the presence of PdCl2(PPh3)2(5%) / CuI/tetrabutylammonium fluoride / triethylamine / tetrahydrofuran (sila-Sonogashira reaction) at room temperature. Copyright Taylor & Francis Group, LLC.
- Zhou, Zhang-Lin,Zhao, Lihua,Zhang, Sean,Vincent, Kent,Lam, Sity,Henze, Dick
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scheme or table
p. 1622 - 1631
(2012/05/05)
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