cas 50820-65-0, Methyl indole-6-carboxylate

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A method of synthesis of indole derivatives
The present invention belongs to the field of indole synthesis technology, in order to solve the current synthesis of indole and its derivatives with ethylene glycol as raw material, the conditions are relatively harsh, the structure of the main catalyst is complex, expensive and other issues, providing a synthesis method of indole derivatives. Pt/Al2O3 catalyst supportingPt/Al2O3was prepared by impregnation with acidicAl2O3as the support, using aniline compounds, ethylene glycol, and the preparedPt/Al2O3 Catalyst for catalytic reaction, control reaction temperature of 190 °C, reaction 24h, after the end of the reaction, first add water to stir evenly, and then with dichloromethane for extraction, organic phase by rotational distillation to remove the solvent, and then with petroleum ether, ethyl acetate as the eluent column chromatography separation, you can obtain the target product. A broad spectrum of the Catalytic System ofPt/Al2O3Supported Catalysts with Good Catalytic Effect inthe Glycol Aniline Reaction was studied, and the substrate range of substituted aniline was mainly expanded.
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Paragraph 0018-0021

(2022/01/10)

2-(1H-INDOLE-3-CARBONYL)-THIAZOLE-4-CARBOXAMIDE DERIVATIVES AND RELATED COMPOUNDS AS ARYL HYDROCARBON RECEPTOR (AHR) AGONISTS FOR THE TREATMENT OF E.G. ANGIOGENESIS IMPLICATED OR INFLAMMATORY DISORDERS
2-(1H-lndole-3-carbonyl)-thiazole-4-carboxamide derivatives and the corresponding imidazole, oxazole and thiophene derivatives and related compounds as aryl hydrocarbon receptor (AHR) agonists for the treatment of angiogenesis implicated disorders, such as e.g. retinopathy, psoriasis, rheumatoid arthritis, obesity and cancer, or inflammatory disorders. The present description discloses the synthesis and characterisation of exemplary compounds as well as pharmacological data thereof (e.g. pages 27 to 32 and 59 to 219; examples 1 to 8; compounds 1-1 to 1-97; tables 1-a, 2 and 3).
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Paragraph 00162; 00311; 00343

(2021/06/26)

Aldehydes as potential acylating reagents for oxidative esterification by inorganic ligand-supported iron catalysis
The oxidative esterification of various aldehydes with alcohols could be achieved by a heterogeneous iron(iii) catalyst supported on a ring-like POM inorganic ligand under mild conditions, affording the corresponding esters, including several drug molecules and natural products, in high yields. ESI-MS and control experiments demonstrated that POM-FeV(O) was the active catalytic species and the plausible mechanism was presented. More importantly, the 6th run of the iron catalyst recycles shows only a slight decrease in the yield.
Yu, Han,Wang, Jingjing,Wu, Zhikang,Zhao, Qixin,Dan, Demin,Han, Sheng,Tang, Jiangjiang,Wei, Yongge
supporting information
p. 4550 - 4554
(2019/08/21)

HEPARANASE INHIBITORS AND USE THEREOF
The invention relates to functionalized quinazoline compounds, pharmaceutical compositions comprising such compounds, and the use of such compounds as heparanase inhibitors for the treatment of diseases or conditions related to heparanse activity.
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Paragraph 0176

(2018/07/05)

Antibacterial compound and its salt
The invention provides a compound of a formula I or a pharmaceutically acceptable salt, a hydrate or a crystal form thereof. An acyl group is connected with the fourth, fifth or sixth-site carbon atom of indolyl. Researches find that the compound provided by the invention has certain antibacterial activity, and can be used as a potential antibacterial drug or daily chemical. Beyond all expectations, a compound 4c is extremely similar to compounds 4a and 4b in structure, but the antibacterial activity of the compound 4c is obviously better than that of the other two compounds; the antibacterial activity of the compound 4c against staphylococcus aureus is significantly better than the antibacterial activity of the compound 4c against escherichia coli, which illustrates that the compound 4c is more sensitive to the staphylococcus aureus; and if being used for antibiosis, the compound 4c can more easily inhibit particular species (such as staphylococcus aureus) in a targeted way, so that the unnecessary drug resistance caused by other bacteria is avoided.
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Paragraph 0031-0035

(2017/10/06)

A double-indole hydrazone compound and use thereof
The invention provides a bisindole acylhydrazone compound shown as the formula I or salt, hydrate or crystals, accepted in the pharmacy, of the bisindole acylhydrazone compound. According to the bisindole acylhydrazone compound, R does not exist or is selected from alkylene of C1-5. The bisindole acylhydrazone compound has a certain antibacterial activity, and can serve as potential antibiotics or a daily chemical product. What is beyond the expectation is that compounds 4e-4h and compounds 4a-4c are quite similar in structure, the antibacterial activity of the compounds 4e-4h and the antibacterial activity of the compounds 4a-4c are obviously better than that of other compounds, particularly, the activity of the compound 4h is best and is remarkably better than that of compounds 4e-4g. The formula I is shown in the specification.
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Paragraph 0036; 0039-0040

(2017/10/06)

A double-indole hydrazone compound and its salt (by machine translation)
The present invention provides a bis-indole compounds shown as formula I hydrazone compound or its pharmaceutically acceptable salt, hydrate or crystalline form. Wherein R is selected from none or C1 - 3 alkylene. This invention discovers, the present invention provides compound has antibacterial activity, can be used as a potential antibacterial drug or of daily use. It is not expected to, compound 4 d with a compound 4a - 4c structure is extremely similar, but its antibacterial activity is obviously superior to other compound; and, compound 4 d to Staphylococcus aureus bacteriostatic activity to be improved to the role of the Escherichia coli, note compound 4 d to Staphylococcus aureus more sensitive, if the use of the compound of antibacterial, in limited under the dosage, more easily targeted inhibit specific bacteria (such as jin pujun), to avoid other bacteria produce unnecessary drug resistance. (by machine translation)
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Paragraph 0032-0038

(2017/10/06)

Novel indole derivative and medicine containing the same (by machine translation)
[A] formation of Amyloid fibrils can be compounds, including therapeutic or prophylactic agent for neurodegenerative disease Amyloid fibrils formation inhibitor compound and of. (I) or its pharmaceutically acceptable compound represented by the formula [a] or a salt or solvate thereof includes the, Amyloid fibrils formation inhibitor. [R1 And R2 Each independently is H, an alkyl group, a cyano group or the like; R3 And R4 Each independently is H, or an alkyl group; R3 And R4 The, joint may form a ring; Ar1 And Ar2 The substituted or unsubstituted heteroaryl group are independently substituted/unsubstituted aryl groups /; X and Y are each independently a single bond, - (=O) - C etc., Z is O or CH2 ; N is an integer of 1 - 3][Drawing] no (by machine translation)
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Paragraph 0306; 0307

(2018/06/30)

five Yuan fragrance heterocyclic structure containing the anti-hepatitis c compound and its preparation and use
The invention discloses an anti-HCV (hepatitis C) compound containing a five-membered heteroaromatic ring structure, as well as a preparation method and applications thereof. The compound has a structure shown as the formula I, the compound has excellent anti-HCV virus activity, can be used for preparing anti-HCV drugs, the prepared drugs can be applied by adopting oral administration, intravenous injection or intramuscular injection.
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Paragraph 0125; 0126-0128

(2016/11/21)

Microwave-assisted synthesis and molecular recognition properties of novel indole acylhydrazone receptors
Indole acylhydrazones were synthesised in high yields under microwave irradiation By using indole carboxylic acid and 1,4-benzenedialdehyde as starting materials. Their structures were characterised by 1H NMR, IR, MS spectra and elemental analysis. Selective recognition properties of these receptors have been investigated by UV-Vis spectra titration indicating that these receptors can form 1:1 supramolecular complexes with malic acid, tartaric acid, ascorbic acid and tryptophan.
Ye, Ying,Suo, Yourui,Yang, Fang,Yang, Yongjing,Han, Lijuan
p. 296 - 299
(2015/06/02)

BETA-LACTAMASE INHIBITORS
Described herein are compounds and compositions that modulate the activity of beta-lactamases. In some embodiments, the compounds described herein inhibit beta-lactamase. In certain embodiments, the compounds described herein are useful in the treatment of bacterial infections.
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Paragraph 0488

(2014/07/22)

Formation of indoles, dihydroisoquinolines, and dihydroquinolines by ruthenium-catalyzed heterocyclizations
Indoles, dihydroisoquinolines, and dihydroquinolines were efficiently prepared by ruthenium-catalyzed heterocyclizations of aromatic homo- and bis-homopropargyl amines/amides in the presence of an amine/ammonium base-acid pair. These regioselective 5-endo and 6-endo cyclizations most probably occur by nucleophilic trapping of key ruthenium-vinylidene intermediates. Georg Thieme Verlag Stuttgart · New York.
Varela-Fernández, Alejandro,Varela, Jesús A.,Saá, Carlos
p. 3285 - 3295
(2013/01/15)

Synthesis of diverse indole libraries on polystyrene resin - Scope and limitations of an organometallic reaction on solid supports
The synthesis of diverse substituted indole structures on solid supports is described. The immobilization of nitrobenzoic acid onto Merrifield resin and the subsequent treatment with alkenyl Grignard reagents delivered indole carboxylates bound to solid s
Knepper, Kerstin,Vanderheiden, Sylvia,Braese, Stefan
experimental part
p. 1191 - 1199
(2012/09/07)

HETEROCYCLIC COMPOUNDS FOR THE INHIBITION OF PASK
Disclosed herein are new heterocyclic compounds and compositions and their application as pharmaceuticals for the treatment of disease. Methods of inhibiting PAS Kinase (PASK) activity in a human or animal subject are also provided for the treatment of diseases such as diabetes mellitus.
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(2012/11/08)

INDOLE COMPOUNDS AND PHARMACEUTICAL USE THEREOF
Provided is an agent for the treatment or prophylaxis of inflammatory diseases, allergic diseases, autoimmune diseases, transplant rejection or the like. A compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, or a solvate thereof: wherein each symbol is as described in the specification.
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Page/Page column 33

(2012/01/03)

Ruthenium-catalyzed cycloisomerization of aromatic homo- and bis-homopropargylic amines/amides: Formation of indoles, dihydroisoquinolines and dihydroquinolines
Ruthenium-catalyzed cycloisomerizations of aromatic homo- and bis-homopropargylic amines/amides efficiently afford indoles, dihydroisoquinolines and dihydroquinolines. These processes were regioselective (5- and 6-endo cyclizations) on using key Ru vinylidene intermediates. The presence of an amine/ammonium base-acid pair increased the rate of cyclization and facilitated the catalytic turnover. Copyright
Varela-Fernandez, Alejandro,Varela, Jesus A.,Saa, Carlos
supporting information; experimental part
p. 1933 - 1937
(2011/10/08)

Substituted Spiroamide Compounds
Substituted spiroamide compounds corresponding to formula (I): wherein A, B, Q1, Q2, Q3, Q4, R1, R8, R9a, R9b, R12, R13, R200 and R210 have defined meanings, processes for their preparation, pharmaceutical compositions containing such compounds, and the use of such compounds for treating or inhibiting pain or other conditions mediated at least in part by the bradykinin 1 receptor (B1R).
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Page/Page column 20

(2010/09/18)

Compounds for the Treatment of Hepatitis C
The invention encompasses compounds of formula I as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV.
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Page/Page column 33

(2008/12/07)

Compounds for the Treatment of Hepatitis C
The invention encompasses compounds of formula I as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV.
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Page/Page column 24

(2008/12/06)

Compounds for the Treatment of Hepatitis C
The invention encompasses compounds of Formula I, pharmaceutically acceptable salts thereof, compositions, and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV.
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Page/Page column 4

(2008/12/07)

Indolobenzazepine HCV NS5B inhibitors
The invention encompasses compounds and salts of Formulas I, II, III, and IV as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV.
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Page/Page column 175

(2008/06/13)

Cyclopropyl fused indolobenzazepine HCV NS5B inhibitors
The invention encompasses compounds of Formula I, pharmaceutically acceptable salts thereof, compositions, and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV.
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Page/Page column 71

(2008/06/13)

IMIDAZOLE DERIVATIVES AS FUNCTIONALLY SELECTIVE ALPHA2C ADRENORECEPTOR AGONISTS
In its many embodiments, the present invention provides imidazole derivatives which are inhibitors of alPha2C adrenergic receptor agonists, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition or amelioration of one or more conditions associated with the alpha2C adrenergic receptors using such compounds or pharmaceutical compositions. Formula (I).
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Page/Page column 37

(2008/06/13)

VIRAL POLYMERASE INHIBITORS
A compound, represented by formula (I) or an enantiomer, diastereoisomer or tautomer thereof : wherein either A or B is nitrogen and the other B or A is C, and the radicals R1, R2, R3, R5, R6, R7, R9, and R10 are as defined herein, or a salt, ester or derivative thereof as viral polymerase inhibitors. The compound is used as an inhibitor of RNA dependent RNA polymerases, particulary those viral polymerases within the Flaviviridae family, more particulary to HCV polymerase.
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Page/Page column 41; 42

(2010/02/15)

VIRAL POLYMERASE INHIBITORS
An enantiomer, diastereoisomer or tautomer of a compound, represented by formula (I): wherein either A or B is nitrogen and the other B or A is C, and the radicals R1, R2, R3, R4, R5, R6, R7, R8, R9, and R10 are as defined herein, or a salt or ester thereof as viral polymerase inhibitors. The compound is used as an inhibitor of RNA dependent RNA polymerases, particularly those viral polymerases within the Flaviviridae family, more particularly to HCV polymerase.
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Page/Page column 49

(2008/06/13)

Antifungal and/or antiparasitic pharmaceutical composition and novel indole derivatives as active principle of such a composition
The present invention relates to novel indole derivatives, their method of preparation and their pharmacological activity as antimycotic and/or antiparasitic compounds.
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Page/Page column 14

(2010/02/06)

INDOLES USEFUL IN THE TREATMENT OF ANDROGEN-RECEPTOR RELATED DISEASES
This invention provides non-steroidal compounds with affinity for the androgen receptor and utility for androgen-receptor related treatments, having a structure according to the formula (1) wherein X is S,SO or S02; R1 is a 5- or 6-membered monocyclic, hetero- or homocyclic, saturated or unsaturated ring structure optionally substituted with one or more substituents selected from the group consisting of halogen, CN, (1C-4C)fluoroalkyl, nitro, (1C-4C)alkyl, (1C-4C)alkoxy or (1C-4C)fluoroalkoxy; R2 is 2-nitrophenyl, 2-cyanophenyl, 2-hydroxymethyl-phenyl, pyridin-2-yl, pyridin-2-yl-N-oxide, 2-benzamide, 2-benzoic acid methyl ester or 2-methoxyphenyl; R3 is H, halogen or (1C-4C)alkyl; R4 is H, OH, (1C-4C)alkoxy, or halogen; R4 is H, OH, (1C-4C)alkoxy, NH2, CN, halogen, (1C-4C)fluoroalkyl, N02, hydroxy(1C-4C)alkyl, C02H, C02(1C-6C)alkyl, or R5 is NHR6, wherein R6 is (1C-6C)acyl optionally substituted with one or more halogens, S(O)2(1C-4C)alkyl, or S(O)2aryl optionally substituted with (1C-4C)alkyl or one or more halogens, or R5 is C(O)N(R8,R9), wherein R8 and R9 each independently are H, (3C-6C)cycloalkyl, or CH2R10, wherein R10 is H, (1C-5C)alkyl, (1C-5C)alkenyl, hydroxy(1C-3C)alkyl, (1C-4C)alkylester of carboxy(1C-4C)alkyl, (1C-3C)alkoxy(1C-3C)alkyl, (mono- or di(1C-4C)alkyl)aminomethyl, (mono- or di(1C-4C)alkyl)aminocarbonyl, or a 3-, 4-, 5- or 6-membered monocyclic, homo- or heterocyclic, aromatic or non-aromatic ring, or R8 and R9 form together with the N a heterocyclic 5- or 6-membered saturated or unsaturated ring optionally substituted with (1C-4C)alkyl; or a salt or hydrate form thereof.
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Page 19

(2010/02/07)

Azaindoles
The invention is directed to compositions containing physiologically active compounds of general formula (I): wherein R1 is aryl or heteroaryl; R2 represents hydrogen, acyl, cyano, halo, lower alkenyl or lower alkyl optionally substituted by a substituent selected from cyano, heteroaryl, heterocycloalkyl, —Z1R8, —C(═O)—NY3Y4, —CO2R8, —NY3Y4, —N(R6)—C(═O)—R7, —N(R6)—C(═O)—NY3Y4, —N(R6)—C(═O)—OR7, —N(R6)—SO2—R7, —N(R6)—SO2—NY3Y4 and one or more halogen a toms ; R3 represents hydrogen, aryl, cyano, halo, heteroaryl, lower alkyl, —C(═O)—OR5 or —C(═O)—NY3Y; and X1 represents N, CH, C-halo, C—CN, C—R7, C—NY3Y4, C—OH, C—Z2R7, C—C(═O)—OR5, C—C(═O)—NY3Y4, C—N(R8)—C(═O)—R7, C—SO2—NY3Y4, C—N(R8)—SO2—R7, C-alkenyl, C-alkynyl or C—NO2; and their prodrugs, and pharmaceutically acceptable salts and solvates of such compounds and their prodrugs, as well as to novel compounds within the scope of formula (I). Such compounds and compositions have valuable pharmaceutical properties, in particular the ability to inhibit protein kinases.
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Page/Page column 113

(2008/06/13)

VIRAL POLYMERASE INHIBITORS
An isomer, enantiomer, diastereoisomer or tautomer of a compound, represented by formula (I): wherein wherein A, B, R2, R3, L, M1, M2, M3, M4, Y1, Y0, Z and Sp are as defined in claim 1, or a salt thereof, as an inhibitor of HCV NS5B polymerase.
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Page 145

(2010/02/07)

Substituted oxoazaheterocyclyl compounds
This invention is directed to oxoazaheterocycyl compounds which inhibit Factor Xa, to oxoazaheterocycyl compounds which inhibit both Factor Xa and Factor IIa, to pharmaceutical compositions comprising these compounds, to intermediates useful for preparing these compounds, to a method of directly inhibiting Factor Xa and to a method of simultaneously directly inhibiting Factor Xa and Factor IIa..
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Page/Page column 73

(2008/06/13)

AGENTS AND METHODS FOR THE TREATMENT OF PROLIFERATIVE DISEASES
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Page 24

(2010/11/30)

Method for inhibiting neoplastic cells with indole derivatives
A method for inhibiting neoplastic cells and related conditions by exposing them to substituted indole derivatives.
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(2008/06/13)

INDOLOYLGUANIDINE DERIVATIVES
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(2008/06/13)

Palladium-Catalyzed Synthesis of Indoles by Reductive N-Heteroannulation of 2-Nitrostyrenes
A palladium-phosphine catalyzed reductive N-heteroannulation of 2-nitrostyrenes, in the presence of carbon monoxide, producing indoles has been developed. Indoles were obtained, in moderate to excellent yield, from substituted 2-nitrostyrenes having either electron-withdrawing (NO2 and CO2-Me) or electron-donating (Br, OH, Me, OMe, and OTf) substituents on the aromatic ring. Best results were obtained using palladium diacetate (6 mol percent) together with triphenylphosphine (24 mol percent) as the catalytic system, under 4 atm of carbon monoxide in acetonitrile at 70 °C. Other palladium(II) and palladium(0) complexes also catalyze the reaction.
So?derberg, Bjo?rn C.,Shriver, James A.
p. 5838 - 5845
(2007/10/03)

Thromboxane A2 synthetase inhibitors with histamine H1-blocking activity: Synthesis and evaluation of a new series of indole derivatives
A novel series of N-substituted 3-(1H-imidazol-1-ylmethyl)indole carboxylic acid derivatives were prepared and evaluated for thromboxane A2 (TXA2) synthetase-inhibitory and histaminergic H1-blocking activity. Among the compounds synthesized, indole-6-carboxylic acid derivatives showed higher activities than the other positional isomers of carboxylic acid. 1-[3-(4- Benzhydryl-1-piperazinyl)propyl]-3-(1H-imidazol-1-ylmethyl)-1H-indole-6- carboxylic acid (12) had the strongest thromboxane synthetase inhibitory activity (IC50 = 5 x 10-8 M) and H1-blocking activity (IC50 = 8 x 10- 9 M).
Kamiya,Matsui,Shirahase,Nakamura,Wada,Kanda,Shimaji,Kakeya
p. 1692 - 1695
(2007/10/03)

1,3,6-Trisubstituted indoles as peptidoleukotriene antagonists: Benefits of a second, polar, pyrrole substituent
1,6-Substituted and 3,5-substituted indoles and indazoles containing acylamino and N-arylsulfonyl amide appendages are potent antagonists of the peptidoleukotrienes LTD4 and LTE4. A compound from the 3,5-substituted indole series, N-[4-[[5-[[(cyclopentyloxy)carbonyl]amino]-1-methylindol-3- yl]methyl]-3-methoxybenzoyl]-2-methyl-benzenesulfonamide (ICI 204,219), is undergoing clinical evaluation for asthma. Two new elements of structural diversity were introduced to this series of antagonists. An investigation of pyrrole substituents in the 1,6-substituted indoles demonstrated that substitution at C-2 was detrimental to biological activity, but the incorporation of hydrophilic groups at C-3 was beneficial. The introduction of a propionamide moiety at C-3 enhanced activity by 1 order of magnitude; N- [4-[[6-(cyclopentylacetamido)-3-[2-(N-methylcarbamoyl)ethyl]indol-1- yl]methyl]-3-methoxybenzoyl]benzenesulfonamide (15c) has a pK(B) of 10.7 at the LTD4 receptor on guinea pig trachea. Modifications of the acylamino portion of the disubstituted antagonists demonstrated that a transposition of the amide CO and NH atoms was viable. N-Cyclopentylmethyl amides in both the 1,6- and 3,5-disubstituted indole series were 1 order of magnitude less potent than the corresponding cyclopentylacetamides. In both series this potency loss could be regained by the incorporation of a propionamide substituent at either C-3 or N-1, respectively. For example, N-[4-[[6-[N- (cyclopentylmethyl)carbamoyl]-3-[2-(pyrrolidin-1-ylcarbonyl)ethyl]indol-1- yl]methyl]-3-methoxybenzoyl]-2-methylbenzenesulfonamide (39c) has a pK(B) of 9.5.
Brown,Cronk,Aharony,Snyder
p. 2419 - 2439
(2007/10/02)

Palladium-Catalyzed Synthesis of Indoles from 2-Nitrostyrenes
In the presence of palladium salts, oxidation of 2-nitrostyrenes 1 with nitrous acid alkyl esters 2 resulted in the formation of 2-nitrophenylacetaldehyde dialkyl acetals 3.Reductive cyclization of the acetals 3 with iron powder in acetic acid afforded indoles 5 in good yield.
Izumi, Taeko,Soutome, Michihiko,Miura, Takashi
p. 1625 - 1629
(2007/10/02)

Indole derivatives and compositions for their use in medicaments
Indole derivative for leukotriene antagonists of the formula STR1 wherein groups A, B, D, E, F & G are as described in the specification.
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(2008/06/13)

Heterocyclic carboxamides
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(2008/06/13)

Aliphatic carboxamides
This invention provides a series of novel heterocyclic aliphatic carboxamides of formula I in which the group >Z--Y--XC=CH--NN--CH=CC=N--NN--N=C and the other radicals have the meanings defined in the following specification. The compounds of formula I are leukotriene antagonists. The invention also provides pharmaceutically acceptable salts of the formula I compounds; pharmaceutical compositions containing the formula I compound, or their salts, for use in the treatment of, for example, allergic or inflammatory diseases, or endotoxic or traumatic shock conditions; and processes for the manufacture of the formula I compounds, as well as intermediates for use in such manufacture.
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(2008/06/13)

Heterocyclic carboxamides
This invention provides a series of novel heterocyclic carboxamides of formula I in which the group --Y--Z is selected from --C(Ra)=C, --N=C, and --CH(Ra)--CH and the other radicals have the meanings defined in the following specification. The compoun
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(2008/06/13)

A Regiocontrolled Synthesis of Substituted Indoles by Palladium-Catalyzed Coupling of 2-Bromonitrobenzenes and 2-Bromoacetanilides
The palladium-catalyzed cross-coupling reaction of 2-bromonitrobenzenes or 2-bromoacetanilides with ethylene has been used to produce a variety of substituted indoles.The mild reaction conditions and selectivity inherent in the coupling reaction have been utilized to produce regiochemically pure 4-, 5-, 6-, and 7-substituted indoles.
Kasahara, Akira,Izumi, Taeko,Murakami, Satoshi,Miyamoto, Kazuhiro,Hino, Toshimi
p. 1405 - 1413
(2007/10/02)

Synthesis of Indole Derivatives from 2-Bromoanilines by a Palladium-assisted Reaction
In the presence of palladium(II) acetate, 2-bromoanilines readily react with enamines such as N-vinylpyrrolidone or α-piperidinostyrene to produce indole derivatives.
Kasahara, Akira,Izumi, Taeko,Kikuchi, Tokio,Xiao-ping Lin
p. 1555 - 1556
(2007/10/02)