- A 5-methyl-pyrrole -2 carboxylic acid ethyl ester preparation method
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The invention discloses a preparation method of ethyl 5-methyl-pyrrol-2 formate, belonging to the technical field of organic synthesis. The preparation method comprises the following steps: preparing ethyl alpha-amino-acetoacetate from glacial acetic acid, ethyl acetoacetate and nitrite solutions used as raw materials; and preparing the ethyl 5-methyl-pyrrol-2 formate from glacial acetic acid, 4,4-dimethoxy-2-butanone, zinc powder and the prepared ethyl alpha-amino-acetoacetate. The synthesis method of the ethyl 5-methyl-pyrrol-2 formate has the advantages of simple synthesis route and high purity of the obtained product. The synthesis method can be used for industrial production, and the yield for one feeding procedure is high, thus being of practical importance for industrialization.
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Paragraph 0023; 0025; 0026
(2017/09/04)
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- SYNTHESIS OF FURAN, THIOPHENE, AND PYRROLES FROM ACETOACETIC ESTERS
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The present invention refers to using ester pgd2 alkylacetoacetoates furan, thiophene, method relates to synthesis of pyrrole, more particularly the acetohydroxy pgd2 ester compound alpha, beta unsaturated carbonyl compounds obtained is added to the 1,5-dicarbonyl compounds (II)/ cobalt manganese (III) method of silica glass by sol the reaction deacetylase with Neel step then alkali to thereby synthesize a compound 1,4-dicarboxylic, Paal-Knorr herein using synthesis on the furan, thiophene, pyrrole for synthesizing relates to method. According to the present invention, a necessary for synthesis of Paal-Knorr 1,4-dicarbonyl compounds efficiently mixed in the oxidation reaction from said 1,5-dicarbonyl compounds (deacetylase reaction) and a conjunction synthesis on the Paal-Knorr in the reaction vessel a are sequentially two reactors furan, thiophene, and of won-port synthesis method by using the mask pattern.. (by machine translation)
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Paragraph 0117-0120
(2016/11/07)
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- Tandem catalytic oxidative deacetylation of acetoacetic esters and heteroaromatic cyclizations
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One pot syntheses of furan, thiophene, and pyrrole were accomplished by oxidative deacetylation using Mn(iii)/Co(ii) catalysts and the Paal-Knorr reaction from 1,5-dicarbonyl compounds, which are prepared from the conjugate addition of ethyl acetoacetate to α,β-unsaturated carbonyl compounds. The oxidative deacetylation and reductive cyclization of β-ketoesters derived from ethyl acetoacetate and o-nitrobenzyl bromides efficiently produced diversely substituted indoles. This journal is
- Ju, Yeming,Miao, Di,Yu, Ruiyang,Koo, Sangho
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p. 2588 - 2599
(2015/04/21)
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- Synthesis and biological evaluation of novobiocin analogues as potential heat shock protein 90 inhibitors
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Recent studies have shown that novobiocin (NB), a member of the coumermycin (CA) family of antibiotics with demonstrated DNA gyrase inhibitory activity, inhibits Heat shock protein 90 (HSP90) by binding weakly to a putative ATP-binding site within its C-terminus. To develop more potent HSP90 inhibitors that target this site and to define structure-activity relationships (SARs) for this class of compounds, we have synthesized twenty seven 3-amido-7- noviosylcoumarin analogues starting from NB and CA. These were evaluated for evidence of HSP90 inhibition using several biological assays including inhibition of cell proliferation and cell cycle arrest, induction of the heat shock response, inhibition of luciferase-refolding in vitro, and depletion of the HSP90 client protein c-erbB-2/HER-2/neu (HER2). This SAR study revealed that a substantial increase in biological activity can be achieved by introduction of an indole-2-carboxamide group in place of 4-hydroxy-isopentylbenzamido group at C-3 of NB in addition to removal/derivatization of the 4-hydroxyl group from the coumarin ring. Methylation of the 4-hydroxyl group in the coumarin moiety moderately increased biological activity as shown by compounds 11 and 13. Our most potent new analogue 19 demonstrated biological activities consistent with known HSP90-binding agents, but with greater potency than NB.
- Gunaherath, G.M. Kamal B.,Marron, Marilyn T.,Wijeratne, E.M. Kithsiri,Whitesell, Luke,Gunatilaka, A.A. Leslie
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p. 5118 - 5129
(2013/09/02)
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- 2-(PIPERIDIN-1-YL)-4-AZOLYL-THIAZOLE-5-CARBOXYLIC ACID DERIVATIVES AGAINST BACTERIAL INFECTIONS
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Compounds of formula (I) and their pharmaceutically acceptable salts are described. Processes for their preparation, pharmaceutical compositions containing them, their use as medicaments and their use in the treatment of bacterial infections are also described
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Page/Page column 70-71
(2010/07/02)
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- 2- (PIPERIDIN-1-YL) -4-HETEROCYCLYL-THIAZOLE-5-CARBOXYLIC ACID DERIVATIVES AGAINST BACTERIAL INFECTIONS
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Compounds of formula (I) and their pharmaceutically acceptable salts are described. Processes for their preparation, pharmaceutical compositions containing them, their use as medicaments and their use in the treatment of bacterial infections are also described. Ring A is selected from formula (a), (b) or (b'):
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Page/Page column 175
(2010/07/02)
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- TRICYCLIC DERIVATIVES OF AZETIDINE AND PYRROLE WITH ANTIBACTERIAL ACTIVITY
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Compounds of formula (I) and their pharmaceutically acceptable salts are described. Processes for their preparation, pharmaceutical compositions containing them, their use as medicaments and their use in the treatment of bacterial infections are also described.
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Page/Page column 54
(2008/06/13)
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- CHEMICAL COMPOUNDS
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Compounds of formula (I) and their pharmaceutically acceptable salts are described: Formula (I). Processes for their preparation, pharmaceutical compositions containing them, their use as medicaments and their use in the treatment of bacterial infections are also described.
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Page/Page column 68
(2010/11/23)
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- CHEMICAL COMPOUNDS
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Compounds of formula (I) and their pharmaceutica11y acceptable salts are described:Processes for their preparation,pharmaceutical compositions containing them, their use as medicaments and their use in the treatment of bacterial infections are also described
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Page/Page column 59
(2008/06/13)
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- ANTIBACTERIAL PIPERIDINE DERIVATIVES
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Compounds of formula (I) and their pharmaceutically acceptable salts are described: Formula (I). Processes for their preparation, pharmaceutical compositions containing them, their use as medicaments and their use in the treatment of bacterial infections are also described.
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Page/Page column 77
(2008/06/13)
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- A new synthesis of pyrroles
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The radical reaction between an N-ethylsulfonylenamide and an α-xanthyl ketone gives an intermediate γ-keto imine which spontaneously ring-closes to the pyrrole.
- Quiclet-Sire, Beatrice,Wendeborn, Frederique,Zard, Samir Z.
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p. 2214 - 2215
(2007/10/03)
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- Synthesis of pyrrole derivatives by palladium-catalyzed cyclization of γ,δ-unsaturated ketone o-pentafluorobenzoyloximes
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Various pyrrole derivatives are synthesized from γ,δ-unsaturated ketone O-pentafluorobenzoyloximes by treatment with catalytic amounts of Pd(PPh3)4 and triethylamine via alkylideneaminopalladium(II) intermediates generated by oxidative addition of the oximes to the Pd(0) complex.
- Tsutsui, Hironori,Kitamura, Mitsuru,Narasaka, Koichi
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p. 1451 - 1460
(2007/10/03)
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- Anion-anion assembly: A new class of anionic supramolecular polymer containing 3,4-dichloro-2,5-diamido-substituted pyrrole anion dimers
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Two molecules containing two 2,5-diamido,3,4-dichloropyrrole units linked via 1,3- or 1,4-substituted benzene rings have been synthesized. The pyrrole groups in these compounds deprotonate in the presence of tetrabutylammonium fluoride and form pyrrole an
- Gale, Philip A.,Navakhun, Korakot,Camiolo, Salvatore,Light, Mark E.,Hursthouse, Michael B.
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p. 11228 - 11229
(2007/10/03)
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- Total synthesis of phorbazole C
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The first total synthesis of the marine natural product phorbazole C 1 occurring in the sea sponge Phorbas aff. clathrata is reported. In the key steps of the convergent approach the 3,4-dichloro-5-ethoxycarbonyl-pyrrole-2-carboxylic acid (4) forms an ami
- Radspieler, Alexander,Liebscher, Jürgen
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p. 4867 - 4871
(2007/10/03)
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- Synthesis of pyrrole derivatives by the heck-type cyclization of γ,δ-unsaturated ketone O-pentafluorobenzoyloximes
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Substituted pyrroles are synthesized from γδ-unsaturated ketone O-pentafluorobenzoyloximes by the intramolecular Heck-type amination of the olefinic moiety catalyzed by Pd(PPh3)4.
- Tsutsui, Hironori,Narasaka, Koichi
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- Synthesis and nucleophilic properties of 1,2 -dialkyl-3-nitropyrroles and 1,5-dialkyl-4-nitropyrrole-2-carboxylic acid derivatives
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1,2-Dialkyl-3-nitropyrroles 1 are versatile synthetic tools for obtaining substituted pyrrolidines or fused ring heterocycles such as pyrrolopyridines, pyrrolopyrimidines or pyrroloazepines. We have established a method for obtaining compounds related to structure 1 and studied the reactivity as a nucleophile of the benzylic type moiety in the alkyl residue bound to position 2.
- Molins-Pujol, Antoni M.,Moranta, Concepcio,Arroyo, Carmina,Rodriguez, M. Teresa,Meca, M. Carmen,Pujol, M. Dolors,Bonal, Joaquim
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p. 2277 - 2289
(2007/10/03)
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- An Improved Synthesis of Pyrroles from N-p-Toluenesulfonylglycine Esters and α,β-Unsaturated Aldehydes and Ketones
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N-p-Toluenesulfonylglycine esters 2 condensed with α,β-unsaturated carbonyl compounds 1 in the presence of the non-nucleophilic base DBU to give hydroxypyrrolidines 3.Dehydration with phosphorous oxychloride-pyridine, followed by DBU mediated elimination
- Lash, Timothy D.,Hoehner, Michael C.
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p. 1671 - 1676
(2007/10/02)
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- SYNTHESIS OF 5-SUBSTITUTED ETHYL PYRROLE-2-CARBOXYLATES
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A new synthesis of 5-substituted ethyl pyrrole-2-carboxylates from ethyl N,N-dibenzylglycinate and β-ketoacetals is described.
- Elder, Todd,Gregory, Lynn C.,Orozco, Arminda,Pflug, Jodi L.,Wiens, P. Scott,Wilkinson, T. J.
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p. 763 - 768
(2007/10/02)
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