- Convenient preparation of primary amides via activation of carboxylic acids with ethyl chloroformate and triethylamine under mild conditions
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Primary amides were easily prepared in 22-99% yields from the corresponding carboxylic acids 1 or 5 with NH4Cl via activation with ClCO 2Et and Et3N. The enantiomers of the corresponding primary amides of Cbz-, Boc-, or Fmoc-α-amino acids can be separated by using a chiral column.
- Noguchi, Takuya,Sekine, Masahiro,Yokoo, Yuki,Jung, Seunghee,Imai, Nobuyuki
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Read Online
- Traceless selenocarboxylates for the one-pot synthesis of amides and derivatives
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We have recently reported a one-pot procedure for glycosyl amides synthesis using selenocarboxylate as traceless reagent. Herein, we present a further application of selenocarboxylate-azide reaction for amide bond formation on a broader range of substrates, including heterocyclic systems and fatty acid. This method proved to be highly efficient for the synthesis of primary and secondary amides, sulfonamides, imides, phosphoramide and also carbamate.
- Silva, Luana,Rosário, Alisson R.,Machado, Bianca M.,Lüdtke, Diogo S.
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supporting information
(2020/12/25)
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- Synthesis and evaluation of α-glucosidase inhibitory activity of sulfonylurea derivatives
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Two series of sulfonylureas derivatives including 24 compounds (4, 7, 5a-5o, 8a-8h), among them 17 new derivatives, have been synthesized and evaluated for their α-glucosidase inhibitory activity. Compounds 5c, 5h and 8e showed significant in vitro α-glucosidase inhibition with IC50 values of 5.58, 79.85 and 213.36 μm, respectively, comparing with the standard compounds acarbose (IC50 = 268.29 μm) and glipizide (IC50 = 300.47 μm). The preliminary structure-activity relationships (SARs) of the synthesized compounds were also investigated.
- Bui, Thi Thoi,Tran, Van Loc,Ngo, Dai Quang,Tran, Van Chien,Tran, Van Sung,Tran, Thi Phuong Thao
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p. 163 - 171
(2021/03/16)
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- Direct observation of a photoinduced nonstabilized nitrile imine structure in the solid state
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(Chemical Equation Presented) We report the direct observation of a bent geometry for a nonstabilized nitrile imine in a metal-coordination crystal. The photoinduced tetrazole ring rupture to release N2 appears to depend on the size of voids around the N3-N4 bond in the crystal lattice. We further observed the selective formation of the 1,3-addition product when a reactive nitrile imine was photogenerated in water. Overall, the bent nitrile imine geometry agrees with the 1,3-dipolar structure, a transient reactive species that mediates the photoinduced 1,3-dipolar cycloaddition in the aqueous medium.
- Zheng, Shao-Liang,Wang, Yizhong,Yu, Zhipeng,Lin, Qing,Coppens, Philip
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supporting information; experimental part
p. 18036 - 18037
(2010/03/31)
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- A convenient method for the preparation of hydroxamic acids
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A one-step conversion of carboxylic acid to hydroxamic acid, under neutral pH conditions is described. This simple, selective and efficient method was applied to a wide range of aliphatic/aromatic carboxylic acid derivatives that contain hydroxyl, halo, ester and other base sensitive groups as substituents. The method utilizes cheaply available reagents and hence it is a practical and cost effective strategy, compared to the other methods available in the literature. (C) 2000 Elsevier Science Ltd.
- Reddy,Kumar,Reddy
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p. 6285 - 6288
(2007/10/03)
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- Synthesis of certain unsubstituted, 9-exo-(dialkylaminomethyl)-, and 9- endo-(aralkyl)-tricyclo [5.2.1.02,6 decane-8-ketoxime esters and ethers with local anesthetic and analgesic activities
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The synthesis of series of unsubstituted, 9-exo-(dialkylaminomethyl)-, and 9-endo-(aralkyl)tricyclo [5.2.1.0(2,6)] decane-8-ketoximes esters and ethers 3a-j, 4a-d, 7a-j and 13a-d from the oxime synthons 2, 6a-e, 12a and 12b, respectively, is described. Al
- Aboul-Enein M, Nabil,El-Azzouny, Aida,Abdallah, Nevine A.,Maklad, Yousreya A.,Saleh, Ola A.,Ebeid
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p. 197 - 208
(2007/10/03)
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- Selective reduction of mixed anhydrides of carboxylic acids to alcohols using borohydride exchange resin (BER)-nickel acetate
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Mixed anhydrides of carboxylic acids have been selectively reduced to alcohols with borohydride exchange resin-nickel acetate under mild conditions and in good yields.
- Bandgar,Modhave,Wadgaonkar,Sande
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p. 1993 - 1994
(2007/10/03)
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- Nickel boride reduction of symmetric and mixed anhydrides of carboxylic acids
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Symmetric and mixed anhydrides of carboxylic acids have been reduced in good yields with nickel boride generated in situ in diglyme.
- Khan, Rahat H.,Rastogi, Ramesh C.
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p. 898 - 900
(2007/10/02)
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- Studies on Quinolizine Derivatives. XXII. Syntheses and Properties of 2-Phenylazacylazine Derivatives
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By the reaction of 6-methyl-4-imino-4H-quinolizine derivatives (5, 8) with the mixed anhydrides (6a-h), 2-phenyl-1-azacylazines (7a-p, 9a-g) were obtained. 2-Phenyl-1,3,6-triazacyclazine derivatives (15a-h, 17a-h, 18a-g) were prepared by the
- Matsuda, Yoshiro,Gotou, Hiromi,Oniyama, Yukio,Katou, Keisuke,Matsumoto, Hiroshi
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p. 4307 - 4315
(2007/10/02)
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- Reduction of Symmetric and Mixed Anhydrides of Carboxylic Acids by Sodium Borohydride with Dropwise Addition of Methanol
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Symmetric and mixed anhydrides of carboxylic acids are reduced in high yields with sodium borohydride in tetrahydrofuran with dropwise addition of methanol.
- Soai, Kenso,Yokoyama, Shuji,Mochida, Katsuko
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p. 647 - 648
(2007/10/02)
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