- A piperazine amide preparation method of the compound (by machine translation)
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The invention discloses a piperazine amides preparation method, comprising: in a solvent, the compound 1 with compound 2 to carry out the reaction, to obtain compound 3, the reaction temperature is 20 °C -120 °C; Ar is substituted or unsubstituted aryl; R is hydrogen, methyl, ethyl, propyl, benzyl, tert-butoxy carbonyl, benzyloxycarbonyl, C1 - C3 Acyl, or substituted or unsubstituted aryl; the aromatic vuill substituted ethylenically C1 - C5 Straight or branched chain alkyl, C1 - C3 Alkoxy, amino, halogen, cyano, aldehyde, C1 - C5 Acyl, trifluoromethyl and carboxyl in the one or more; the aromatic substituent is phenyl, thienyl, pyrrolyl, pyrimidinyl or pyridinyl. Preparation method of this invention mild condition, raw material properties are stable, easy to use and storage, high yield, the process is simple, low requirements on equipment, after treatment is convenient, product separation and purification is simple. (by machine translation)
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Paragraph 0031-0033
(2017/08/25)
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- Highly efficient preparation of amides from aminium carboxylates using N-(p-toluenesulfonyl) imidazole
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Treatment of aminium carboxylates with N-(p-toluenesulfonyl)imidazole in the presence of triethylamine in DMF at 100 °C afforded the corresponding amides in good to excellent yields. N-(p-Toluenesulfonyl)imidazole proved to be a highly efficient coupling reagent for the preparation of numerous structurally diverse primary, secondary and tertiary amides.
- Behrouz, Somayeh,Rad, Mohammad Navid Soltani,Forouhari, Elham
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p. 101 - 106
(2016/03/08)
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- Dehydrogenative amide synthesis from alcohol and amine catalyzed by hydrotalcite-supported gold nanoparticles
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Hydrotalcite-supported nano-gold (Au/HT) was found to be a highly efficient heterogeneous catalyst for the dehydrogenative synthesis of amide from alcohol and amine. Amines and alcohols with different structures could be converted into the amides under mild reaction conditions with up to 98% isolated yields. Mechanism exploration suggested that ester might be the reaction intermediate.
- Zhu, Jiangling,Zhang, Yan,Shi, Feng,Deng, Youquan
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supporting information; experimental part
p. 3178 - 3180
(2012/07/31)
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- Efficient and chemoselective alkylation of amines/amino acids using alcohols as alkylating reagents under mild conditions
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We report a mild and environmentally benign method for the synthesis of tertiary amines using alcohols as the alkylating reagents. Not only secondary amines such as piperazines but also amino acids and amino alcohols can be N-alkylated selectively. For N,O-benzyl protected amino alcohols, both N,O-de-benzylation and N-methylation were achieved in one-pot. The Royal Society of Chemistry.
- Xu, Chu-Pei,Xiao, Zhen-Hua,Zhuo, Bi-Qin,Wang, Yu-Huang,Huang, Pei-Qiang
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supporting information; experimental part
p. 7834 - 7836
(2010/11/24)
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- Discovery and biological evaluation of adamantyl amide 11β-HSD1 inhibitors
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A series of adamantyl amide 11β-HSD1 inhibitors has been discovered and chemically modified. Selected compounds are selective for 11β-HSD1 over 11β-HSD2 and possess excellent cellular potency in human and murine 11β-HSD1 assays. Good pharmacodynamic characteristics are observed in ex vivo assays.
- Webster, Scott P.,Ward, Peter,Binnie, Margaret,Craigie, Eilidh,McConnell, Kirsty M.M.,Sooy, Karen,Vinter, Andy,Seckl, Jonathan R.,Walker, Brian R.
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p. 2838 - 2843
(2008/02/05)
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- Unique spirocyclopiperazinium salt I: Synthesis and structure-activity relationship of spirocyclopiperazinium salts as analgesics
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Based on the structure of compound 3, two series of spirocyclopiperazinium derivatives 7a-n and 10a-h were synthesized and evaluated for their in vivo analgesic and sedative activities. Compounds 7f and 10c were discovered to exhibit excellent analgesic activity. Structure-activity relationships revealed that anion of the quaternary salt affected the analgesic and sedative activity significantly; the allyl group is a most effective group among the compounds 7a-n; the electron-released substitute on the aromatic ring is favorable to increase the analgesic activity.
- Gao, Feng-Li,Wang, Xin,Zhang, Hong-Mei,Cheng, Tie-Ming,Li, Run-Tao
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p. 1535 - 1537
(2007/10/03)
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- Microwave-assisted solvent-free parallel synthesis of thioamides
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Rapid parallel synthesis of thioamides is described. A library of amides, synthesised by mixing acyl chlorides and diamines, was transformed into the corresponding thioamides utilising Lawesson's reagent as the oxygen/sulphur exchange reagent. Purification by solid-phase extraction afforded the library members in adequate purities and yields. (C) 2000 Elsevier Science Ltd.
- Olsson,Hansen,Andersson
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p. 7947 - 7950
(2007/10/03)
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