A series of N1-substituted-3-aryl-4-alkyl-4, 5-dihydro-1H-1-pyrazolethiocarboxamide were prepared from the Mannich bases of aryl ketones in good yields. Some derivatives were found to be active against the cysteine p...A series of N1-substituted-3-aryl-4-alkyl-4, 5-dihydro-1H-1-pyrazolethiocarboxamide were prepared from the Mannich bases of aryl ketones in good yields. Some derivatives were found to be active against the cysteine protease of T.cruzi..展开更多
The reaction of phenacyl benzoate derivatives with acetamide at about 140°in the presence of BF3 catalyst gave 2-aryl-4-phenyloxazoles. This method can be applied to the preparation of 2-alkyl-4-phenyloxazoles as...The reaction of phenacyl benzoate derivatives with acetamide at about 140°in the presence of BF3 catalyst gave 2-aryl-4-phenyloxazoles. This method can be applied to the preparation of 2-alkyl-4-phenyloxazoles as well.展开更多
In order to investigate the biological activity of novel bis-pyrazole compounds, a series of N-（3-alkyl-5-（N-methylcarbamyl）- 1H-pyrazol-4-yl）-3-alkyl-4-substituted-lH-pyrazole-5-carboxamides were designed and syn...In order to investigate the biological activity of novel bis-pyrazole compounds, a series of N-（3-alkyl-5-（N-methylcarbamyl）- 1H-pyrazol-4-yl）-3-alkyl-4-substituted-lH-pyrazole-5-carboxamides were designed and synthesized with ethyl 3-alkyl-lH-pyr- azole-5-carboxylate 1 as starting materials. N-Methyl-3-alkyl-4-amino-lH-pyrazole-5-carboxamides 6 were obtained from 1 via 5 steps. 3-Alkyl-4-substitued-lH-pyrazole-5-carboxyl chlorides 4a, 4b, lla, llb, llc or 12 were also obtained from 1 via several steps. Target compounds 7a-Tg were obtained after the reaction of 6 with the above 1H-pyrazole-5-carboxyl chlorides. Preliminary bioassay showed some compounds possessing good inactivation effect against TMV （tobacco mosaic virus）. Compound 7a showed higher activity superior to ningnanmycin at a concentration of 5.0 × 10^-4 g/mE and equal activity at 1.0 × 10^-4 g/mE; 7b and 7c showed equal activity to virazole both at concentrations of 5.0 × 10^-4 g/mE and 1.0 × 10^-4 g/mL.展开更多
Ethyl 3-alkyl-4-hydroxy-2-thioxothiazolidine-4-carboxylates were prepared in excellent yields from the reaction of corresponding primary amines with carbon disulfide and ethyl 3-bromo-2-oxopropanoate in the presence o...Ethyl 3-alkyl-4-hydroxy-2-thioxothiazolidine-4-carboxylates were prepared in excellent yields from the reaction of corresponding primary amines with carbon disulfide and ethyl 3-bromo-2-oxopropanoate in the presence of anhydrous potassium phosphate in DMF at room temperature within 1 h. The structures of the highly functionalized products were corroborated spectroscopically （IR, ^1H NMR, ^13C NMR, EI-MS） and by elemental analyses. A plausible mechanism for such type of cyclization was proposed.展开更多
A Lewis acid-catalyzed[4+2]cycloaddition of 3-alkyl-2-vinylindoles withβ,γ-unsaturatedα-ketoesters has been established in the presence of Sc(OTf)3,which afforded a series of indole-containing pyran derivatives in ...A Lewis acid-catalyzed[4+2]cycloaddition of 3-alkyl-2-vinylindoles withβ,γ-unsaturatedα-ketoesters has been established in the presence of Sc(OTf)3,which afforded a series of indole-containing pyran derivatives in generally good yields(up to 90%yield)with excellent diastereoselectivities(up to >95:5 dr)under mild conditions.This approach not only enriches the chemistry of 3-alkyl-2-vinylindoles,but also has provided an atom-economic method for the synthesis of indole-containing pyran derivatives with potential bioactivity.展开更多
文摘A series of N1-substituted-3-aryl-4-alkyl-4, 5-dihydro-1H-1-pyrazolethiocarboxamide were prepared from the Mannich bases of aryl ketones in good yields. Some derivatives were found to be active against the cysteine protease of T.cruzi..
文摘The reaction of phenacyl benzoate derivatives with acetamide at about 140°in the presence of BF3 catalyst gave 2-aryl-4-phenyloxazoles. This method can be applied to the preparation of 2-alkyl-4-phenyloxazoles as well.
基金the National Natural Science Fund of China(No.20902107)the Fundamental Research Fund for the Central Universities(No.2011JS033)
文摘In order to investigate the biological activity of novel bis-pyrazole compounds, a series of N-（3-alkyl-5-（N-methylcarbamyl）- 1H-pyrazol-4-yl）-3-alkyl-4-substituted-lH-pyrazole-5-carboxamides were designed and synthesized with ethyl 3-alkyl-lH-pyr- azole-5-carboxylate 1 as starting materials. N-Methyl-3-alkyl-4-amino-lH-pyrazole-5-carboxamides 6 were obtained from 1 via 5 steps. 3-Alkyl-4-substitued-lH-pyrazole-5-carboxyl chlorides 4a, 4b, lla, llb, llc or 12 were also obtained from 1 via several steps. Target compounds 7a-Tg were obtained after the reaction of 6 with the above 1H-pyrazole-5-carboxyl chlorides. Preliminary bioassay showed some compounds possessing good inactivation effect against TMV （tobacco mosaic virus）. Compound 7a showed higher activity superior to ningnanmycin at a concentration of 5.0 × 10^-4 g/mE and equal activity at 1.0 × 10^-4 g/mE; 7b and 7c showed equal activity to virazole both at concentrations of 5.0 × 10^-4 g/mE and 1.0 × 10^-4 g/mL.
基金Project supported by the National Natural Science Foundation of China （Nos. 20172006 and 20472008）.
文摘Ethyl 3-alkyl-4-hydroxy-2-thioxothiazolidine-4-carboxylates were prepared in excellent yields from the reaction of corresponding primary amines with carbon disulfide and ethyl 3-bromo-2-oxopropanoate in the presence of anhydrous potassium phosphate in DMF at room temperature within 1 h. The structures of the highly functionalized products were corroborated spectroscopically （IR, ^1H NMR, ^13C NMR, EI-MS） and by elemental analyses. A plausible mechanism for such type of cyclization was proposed.
基金This work was supported by National Natural Science Foundation of China(No.21772069)Natural Science Foundation of Jiangsu Province(No.BK20201018)+1 种基金Undergraduate Students Project of Jiangsu Province(No.202010320050Z)High-level Innovative and Entrepreneurial Talents Introduction Plan of Jiangsu Province,and Natural Science Foundation of JSNU(No.19XSRX010).
文摘A Lewis acid-catalyzed[4+2]cycloaddition of 3-alkyl-2-vinylindoles withβ,γ-unsaturatedα-ketoesters has been established in the presence of Sc(OTf)3,which afforded a series of indole-containing pyran derivatives in generally good yields(up to 90%yield)with excellent diastereoselectivities(up to >95:5 dr)under mild conditions.This approach not only enriches the chemistry of 3-alkyl-2-vinylindoles,but also has provided an atom-economic method for the synthesis of indole-containing pyran derivatives with potential bioactivity.
