- Method of preparing 4,5-disubstituted 1,2,3-triazole with pyridinium salt
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The invention relates to a method of synthesizing a 4,5-disubstituted 1,2,3-triazole compound. The method comprises the following step of by taking pyridine, halohydrocarbon, sulfonic ester, aldehydeand sodium azide as raw materials, and performing room-temperature reaction with a one-pot method. The synthetic method does not need a metal-containing catalyst, has the advantages of high yield of synthetic products, mild reaction condition, good functional group compatibility and the like, is simple in operation step, mild in reaction condition and wide in application range of a substrate, hasinnovativeness and a potential practical value and is suitable for industrial production.
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Paragraph 0033-0034
(2018/09/08)
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- Practical one-pot syntheses of ethyl 4-substituted-1 H-pyrrole-3- carboxylates from aldehydes
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Ethyl 4-substituted-1H-pyrrole-3-carboxylates were prepared in a one-pot manner starting from aromatic or aliphatic aldehydes via a Horner-Wadsworth- Emmons reaction and subsequent reaction with tosylmethylisocyanide (TosMIC) in the presence of sodium tert-amylate in toluene. Judicious selection of base and solvent led to the use of a single solvent, i.e., toluene, for reactions as well as for crystallization to render the one-pot process more practical and greener than the stepwise version. hisin@ lels.com.
- Chang, Jay Hyok,Shin, Hyunik
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p. 291 - 293
(2013/01/03)
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- N-(1-naphthylmethyl)-N-(1-alkyl-4-aryl-1H-pyrrol-3-yl methyl)methylamines related to naftifine. Synthesis and antifungal activity
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Various pyrrole analogues of the antifungal drug naftifine were prepared starting from cinnamates via the tosylmethylisocyanide (TosMIC) reaction. After alkylation and hydrolysis, the intermediate arylpyrrole esters afforded 1-alkyl-4-aryl-1H-pyrrole-3-carboxylic acids, which were condensed with N-(1-naphthylmethyl)methylamine in the presence of EDCI and triethylamine. The related amides were then reduced with lithium aluminum hydride to the required N-(1-naphthylmethyl)-N-(1-alkyl-4-aryl-1H-pyrrol-3-ylmethyl)methylamines. The new compounds were evaluated for antifungal activity in comparison with naftifine and other imidazole drugs used in the clinic. Derivative 7c was active against Candida parapsilosis and compound 51 against Candida albicans. Weak activity against dermatophytes was shown by a number of derivatives. Moreover, compounds 4g, 4j, 4k and 4p were found active against Staphylococcus aureus with potencies comparable to that of streptomycin.
- Di Santo, Roberto,Costi, Roberta,Artico, Marino,Massa, Silvio,Musiu, Chiara,Milia, Carlo,Putzolu, Monica,La Colla, Paolo
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