- An efficient one pot synthesis of carbamate esters through alcoholic tosylates
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An efficient O-alkylation of alcoholic tosylates with amines in a K2CO3/CO2 system in the presence of tetrabutyl ammonium iodide (TBAI) provides exclusive formation of carbamates.
- Chaturvedi, Devdutt,Kumar, Atul,Ray
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Read Online
- Method for preparing N,N-Dimethylaniline compound through alkylation of alkyl tosylate
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The invention provides a method for preparing a N,N-Dimethylaniline compound through alkylation of alkyl tosylate, and belongs to the technical field of organic synthesis. According to the method, paratoluensulfonyl chloride and fatty alcohol serve as raw materials, pyridine serves as an acid-binding agent, and the alkyl tosylate is generated; the alkyl tosylate as an alkylation reagent and an aniline compound are alkylated under the alkaline condition to obtain the N,N-Dimethylaniline compound. The method is implemented at normal pressure, the operation is simple, no waste acid is generated,the yield and the purity are high, and the method is suitable for industrial and scaled production.
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Paragraph 0085; 0086
(2019/07/11)
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- 2-AMINO-QUINOLINE DERIVATIVES
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Described herein are 2-amino-quinoline derivatives that are agonists of toll-like receptors 7 and 8 (TLR7/8), pharmaceutical compositions, and methods of use of the compounds and compositions to treat various diseases, such as viral, cancer, and allergic diseases, in need thereof by administering a therapeutically effective amount of a 2-amino-quinoline derivative.
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Paragraph 0174; 0204; 0205-0206
(2018/11/22)
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- Ionic liquid brush as an efficient and reusable heterogeneous catalytic assembly for the tosylation of phenols and alcohols in neat water
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A very efficient and reusable heterogeneous ionic liquid brush assembly was developed. The catalyst exhibits high catalytic activity for the tosylation of phenols and alcohols in neat water. Moreover, the catalyst shows outstanding stability and reusability, and it can be simply and effectively recovered and reused five times without noticeable loss of catalytic activity.
- Feng, Simin,Li, Jing,Wei, Junfa
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supporting information
p. 4743 - 4746
(2017/07/12)
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- An efficient practical tosylation of phenols, amines, and alcohols employing mild reagent [DMAPTs]+Cl?
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Efficient exploration of [DMAPTs]+Cl?for base free and chromatography free preparation of sulfonate esters from phenols and alcohols and sulfonamides from amines was achieved in excellent yields. Majority of the phenols irrespective of their substituents electronic nature underwent tosylation nearly at same reaction rate with an average yield of 95%. For amines, ring activating substituents favors rapid sulfonylation while the ring deactivating substituents relatively lowers the rate of tosylation. Furthermore the reagent was employed for Chemoselective sulfonylation as well as solvent free tosylation of phenols and amines.
- Dhonthulachitty, Chiranjeevi,Kothakapu, Sridhar Reddy,Neella, Chandra Kiran
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supporting information
p. 4620 - 4623
(2016/09/23)
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- Peptide deformylase inhibitors with retro-amide scaffold: Synthesis and structure-activity relationships
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Peptide deformylase (PDF) is a metalloprotease catalyzing the removal of a formyl group from newly synthesized proteins. Thus inhibition of PDF activity is considered to be one of the most effective antibiotic strategies. Reported herein are the synthesis
- Lee, Seung Kyu,Choi, Kwang Hyun,Lee, Sang Jae,Suh, Se Won,Kim, B. Moon,Lee, Bong Jin
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body text
p. 4317 - 4319
(2010/10/03)
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- Stereoselective synthesis of bioactive isosteviol derivatives as α-glucosidase inhibitors
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Considerable interest has been attracted in isosteviol and its derivatives because of their large variety of pharmacological activities. In this project, a series of novel compounds containing hydroxyl, hydroxymethyl group and heteroatom-containing frameworks fused with isosteviol structure were synthesized and evaluated as α-glucosidase inhibitors, aimed at clarifying the structure-activity correlation. The results indicated that these isosteviol derivatives were capable of inhibiting in vitro α-glucosidase with moderate to good activities. Among them, indole derivative 15b exhibited the highest activities and thus may be exploitable as a lead compound for the development of potent α-glucosidase inhibitors.
- Wu, Ya,Yang, Jing-Hua,Dai, Gui-Fu,Liu, Cong-Jun,Tian, Guo-Qiang,Ma, Wen-Yan,Tao, Jing-Chao
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experimental part
p. 1464 - 1473
(2009/09/05)
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- Silver(I) oxide-mediated facile and practical sulfonylation of alcohols
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Primary and secondary alcohols were efficiently sulfonylated in the presence of silver(I) oxide and potassium iodide in dichloromethane. The sulfonylation occurs under mild, neutral reaction conditions. The ease of isolation of the final product presents a marked advantage over the known methodologies.
- Bouzide, Abderrahim,LeBerre, Nicolas,Sauvé, Gilles
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p. 8781 - 8783
(2007/10/03)
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