Abstract: Methods for the synthesis of an indole in provided. Methods comprise oxidizing a N-aryl imine in the presence of a palladium-based catalyst, an oxidant, and a solvent.

Abstract: The present invention relates to a chemical process for the manufacture of a compound of Formula II

Abstract: The present invention relates to processes for preparing indoline derivatives, particularly 1-acetyl-6-amino-3,3-dimethyl-2,3-dihydroindole.

Abstract: The present invention relates to processes for preparing indoline derivatives, particularly 1-acetyl-6-amino-3,3-dimethyl-2,3-dihydroindole.

Abstract: An isomer, enantiomer, diastereoisomer, or tautomer of a compound, represented by formula I: wherein: A is O, S, NR1, or CR1, wherein R1 is defined herein; — represents either a single or a double bond; R2 is selected from: H, halogen, R21, OR21, SR21, COOR21, SO2N(R22)2, N(R22)2, CON(R22)2, NR22C(O)R22 or NR22C(O)NR22 wherein R21 and each R22 is defined herein; B is NR3 or CR3, with the proviso that one of A or B is either CR1 or CR3, wherein R3 is defined herein; K is N or CR4, wherein R4 is defined herein; L is N or CR5 wherein R5 has the same definition as R4 defined above; M is N or CR7, wherein R7 has the same definition as R4 defined above; Y1 is O or S; Z is N(R6a)R6 or OR6, wherein R6a is H or alkyl or NR61R62 wherein R61 and R62 are defined herein; a salt or a derivative thereof, as an inhibitor of HCV NS5B polymerase.

Abstract: There is provided a novel process for producing an indole derivative which comprises cyclizing 2-nitrobenzylcarbony compound in the presence of a catalyst comprising a Group VIII metal of the Periodic Table, characterized by conducting the cyclization in a gas atmosphere containing carbon monoxide. The process enables an indole compound to be selectively produced in a high yield from 2-nitrobenzylcarbonyl compound, and hardly yields an indoline compound as a reduction by-product that has been a problem in the catalytic hydrogenation method employing a noble metal catalyst. The indole derivative produced by the present process is useful for various fine chemical intermediates including compounds and physiologically active substances such as pharmaceuticals and agrochemicals.

Abstract: A method for the preparation of 5-benzyloxy-2-(4-benzyloxyphenyl)-3-methyl-1H-indole of formula (1) by reaction of 2-bromo-4?-benzyloxypropiophenone and 4-benzyloxyaniline hydrochloride, in which high purity of the product is achieved by isolation of the intermediate, N-(4-benzyloxyphenyl)-?-amino-4-benzyloxypropiophenone of formula (10), in the solid state. The method may be used for the preparation of bazedoxifen of formula (2).

Abstract: The present invention relates to a coupling method between intramolecular carbon using the intramolecular cyclization reaction in situ of an allyl-indium compound derived from an allyl derivative containing an unsaturated hydrocarbon compound and indium, in presence of a transition metal compound catalyst. More particularly, the present invention relates to a coupling method between intramolecular carbon for preparing a cyclic compound having a vinyl group as a substituent by bonding a carbon in an allyl derivative containing an unsaturated hydrocarbon compound and a carbon in the unsaturated hydrocarbon compound via intramolecular cyclization reaction in situ of an allyl-indium compound as a coupling agent derived from the allyl derivative containing the unsaturated hydrocarbon and indium (In), in presence of a palladium catalyst.

Abstract: An isomer, enantiomer, diastereoisomer, or tautomer of a compound, represented by formula I: wherein: A is O, S, NR1, or CR1, wherein R1 is defined herein; ----- represents either a single or a double bond; R2 is selected from: H, halogen, R21, OR21, SR21, COOR21, SO2N(R22)2, N(R22)2, CON(R22)2, NR22C(O)R22 or NR22C(O)NR22 wherein R21 and each R22 is defined herein; B is NR3 or CR3, with the proviso that one of A or B is either CR1 or CR3, wherein R3 is defined herein; K is N or CR4, wherein R4 is defined herein; L is N or CR5, wherein R5 has the same definition as R4 defined above; M is N or CR7, wherein R7 has the same definition as R4 defined above; Y1 is O or S; Z is N(R6a)R6 or OR6, wherein R6a is H or alkyl or NR61R62 wherein R61 and R62 are defined herein; a salt or a derivative thereof, as an inhibitor of HCV NS5B polymerase.

Abstract: The present invention provides a method for making substituted indole compounds of general formula III comprising the step of: (a) reacting a 2-bromoaniline or 2-chloroaniline of general formula (I) (I) wherein: X, R and R1 are defined herein with a substituted acetylene of formula (II) wherein R2 and R3 are defined herein in the presence of a palladium catalyst, a ligand, and a base in a solvent at a suitable temperature to give a compound of formula (III);

Abstract: The present invention relates to a ?3 adrenergic receptor agonist of formula (I); or a pharmaceutical salt thereof; which is capable of increasing lipolysis and energy expenditure in cells and, therefore, is useful for treating Type 2 diabetes and/or obesity.

Abstract: The invention provides processes for the preparation of fused pyrroles, preferably indoles, which permit the use of inexpensive aromatic amines themselves as the raw material and attain high atomic efficiency and high regioselectivity. Specifically, a process for the preparation of fused pyrroles, e.g., indoles bearing methyl at the 3-position of pyrrole ring and R1 (or R2) of the general formula (4) at the 2-position thereof, or 3,3-disubstituted indoles bearing R1 and R2 at the 3-position of pyrrole ring and methyl at the 2-position thereof, characterized by reacting an alkynol of the general formula (4) with an aromatic primary amine in the presence of a ruthenium complex, more preferably with an acid or an ammonium salt thereof being made to coexist. [In the general formula (4), R1 and R2 are each independently hydrogen, optionally substituted alkyl, or optionally substituted aryl, or alternatively R1 and R2 may be united to form an alkylene chain.

Abstract: A process for the preparation heterocyclic indene analogs, especially with the preparation of 4-hydroxycarbazole or N-protected 4-hydroxycarbazole, involves cyclocarbonylation followed by saponification. This process avoids high temperatures and high catalyst loadings.

Abstract: The invention provides processes for the preparation of fused pyrroles, preferably indoles, which permit the use of inexpensive aromatic amines themselves as the raw material and attain high atomic efficiency and high regioselectivity. Specifically, a process for the preparation of fused pyrroles, e.g., indoles bearing methyl at the 3-position of pyrrole ring and R1 (or R2) of the general formula (4) at the 2-position thereof, or 3,3-disubstituted indoles bearing R1 and R2 at the 3-position of pyrrole ring and methyl at the 2-position thereof, characterized by reacting an alkynol of the general formula (4) with an aromatic primary amine in the presence of a ruthenium complex, more preferably with an acid or an ammonium salt thereof being made to coexist.

Abstract: Disclosed are methods of synthesizing libraries of diverse complex hexahydroisoindole, hexahydroisooxyindole and octahydroisooxyquinoline compounds through the use of a facile intramolecular Diels Alder reaction. The invention is further directed to methods for synthesizing the libraries on solid supports. The invention is further directed to methods for identifying and isolating such hexahydroisoindole, hexahydroisooxyindole and octahydroisooxyquinoline compounds with useful and diverse activities from such libraries.

Abstract: The present invention relates to a process for the preparation of indoles.

Abstract: A process for the preparation heterocyclic indene analogs, especially with the preparation of 4-hydroxycarbazole or N-protected 4-hydroxycarbazole, involves cyclocarbonylation followed by saponification. This process avoids high temperatures and high catalyst loadings.

Abstract: The subject invention involves a solid-phase process for the synthesis of indole compounds comprising the steps:

Abstract: The present application describes a process for preparing compounds of the indole type of the formula 1

Abstract: The invention provides a novel amino acid, neo-tryptophan, as well as polypeptides containing this novel amino acid such as neurotensin analogs. In addition, the invention provides neo-tryptophan derivatives, serotonin-like neo-tryptophan derivatives, and polypeptides containing such derivatives. The invention also provides methods for making neo-tryptophan, neo-tryptophan derivatives, serotonin-like neo-tryptophan derivatives, and compositions containing these compounds. Further, the invention provides methods for inducing a neurotensin response in a mammal as well as methods for treating a mammal having a serotonin recognition molecule.

Abstract: A process for the preparation of 5,6-disubstituted indoles in which a 4-5-disubstituted-2,.beta.-nitrostyrene is subjected to a reductive cyclization in the presence of a water soluble dithionite salt.

Abstract: Disclosed is a method of preparing a compound represented by the following structural formula: ##STR1## and physiological salts thereof. R.sup.1 is --H, an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group.R.sup.2 is a substituted or unsubstituted 2-hydroxy-1-ethyl group.Ring A is a substituted or unsubstituted aryl group.Ring B is substituted or unsubstituted at position two.

Abstract: A process for preparing 1H-indole-3-glyoxamides useful for inhibiting SPLA.sub.2 and novel intermediates useful in the preparation of such compounds.

Abstract: The present invention is directed to the synthesis of useful products from the explosive trinitrotoluene. This substance has a limited shelf life as a reliable explosive and large quantities of it have and will become surplus. Ecologically safe, and preferably commercially useful ways of disposing of it are therefore much to be desired. In the present invention the end products are nitroindoles of the general formula 4-Z.sup.1,6-Z.sup.2 indole wherein Z.sup.1 and Z.sup.2 are the same or different and are halo or nitro provided at least one of said groups is nitro.

Abstract: The present invention relates to novel substituted indole compounds of formula (I) ##STR1## having pharmacological activity, to processes for their preparation, to solid phase methods for preparing libraries of the compounds, to utilizing libraries of the compounds for drug discovery, and to pharmaceutical compositions thereof.

Abstract: Binuclear iridium (I) phosphine complexes of the general formula: ##STR1## in which X is fluorine, chlorine, bromine or iodine, and ##STR2## is in each case a chiral bidentate diphosphine ligand. The complexes are particularly suitable as catalysts for the inter- or intramolecular asymmetric hydroamination of prochiral olefins.

Abstract: A process for preparing libraries of indole compounds by solid phase synthesis in the presence of organometallic catalysts. The resulting compounds have a very high purity degree, which allows biological testing on the crude products with a high confidence degree, without any cross contaminations.

Abstract: The present invention is directed to the preparation of an aqueous hair dyeing composition containing an effective hair dyeing amount--at least 2 mg/ml--5,6-dihydroxyindole (DHI). An aqueous hair dyeing composition is produced by reacting under essentially anaerobic conditions dopa or a salt thereof with an alkali metal ferricyanide oxidant in an aqueous reaction medium to obtain dopachrome, and permitting the dopachrome to undergo rearrangement in the aqueous medium to form 5,6-dihydroxyindole, said rearrangement being conducted in the substantial absence of oxidant, the aqueous medium being buffered by sufficient buffering agent to maintain a pH of from about 4.5 to about 9 for the reaction medium throughout the series of reactions that take place thereafter, removing the ferrocyanide species present in the aqueous system, and lastly, charging the composition into a suitable container.

Abstract: Disclosed is a process for the preparation of a novel class of 1-hydroxy-6-organosulphonylindoles comprising catalytically hydrogenating beta-dimethylamino-2-nitro-4-organosulphonylstyrenes.

Abstract: A method of producing and isolating 5,6-diacetoxyindole (DAI) in a single reaction vessel comprising the following steps:(a) preparing a first solution comprising dopa, water and a solubilizing agent selected from the group consisting of an acid having a pk.sub.a value equal to or less than 4 and a first base having a pk.sub.b value equal to or greater than 10;(b) preparing a second solution comprising an oxidant, a buffer and water;(c) mixing the first and second solutions to form a combined solution which is rendered oxygen-free and has a pH of from about 6 to about 9;(d) stirring the combined solution in an inert atmosphere until 5,6-dihydroxyindole (DHI) is substantially completely formed;(e) adding a derivatizing agent and a second base to the combined solution to form a final solution;(f) stirring the final solution until the DHI is substantially fully consumed;(g) cooling the final solution to precipitate DAI;(h) isolating the precipitated DAI.

Abstract: The present invention relates to a novel process for the preparation of heterocyclic alkylamide derivatives having the following formula: ##STR1## and the pharmaceutically acceptable acid addition salt thereof wherein X represents halo, alkyl having 1 to 6 carbon atoms, hydrido, trifluoromethyl, phenyl, or lower alkoxy having 1 to 6 carbon atoms; Y represents the group --CN or --CONH.sub.2 ; R.sub.2 represents alkyl having 1 to 6 carbon atoms; R.sub.

Abstract: Process for the preparation of 5,6-dihydroxyindole, wherein the compound of formula: ##STR1## in which R' denotes a hydrogen atom or an optionally substituted benzyl radical, is subjected either to the action of hydrogen under pressure or to a hydrogen transfer operation, in a solvent medium and in the presence of a hydrogenation catalyst.

Abstract: The present invention is a cyclization process utilizing the catalyst copper aluminum borate which process comprises the step of contacting (1) a compound having a fragment in which a carbon-containing chain of at least three atoms in sequence is bonded at one end thereof to a nitrogen, oxygen, or sulfur atom, and at the opposite end to a carbon, nitrogen, oxygen, or sulfur atom, where the latter are bonded to at least one hydrogen atom; with (2) a catalyst comprising at least one member selected from the group consisting of copper aluminum borate and zero valent copper on a support comprising aluminum borate, under conditions sufficient to effect ring closure between the ends of the fragment to obtain a compound comprising a heterocyclic ring.

Abstract: An indole of the formula ##STR1## wherein R.sub.5 and R.sub.6 are acetoxy or hydrogen, at least one of R.sub.5 and R.sub.6 being acetoxy, is prepared, in good yield, in a one pot synthesis, without extraction, recrystallization or isolation of intermediate reaction product; A compound of the formula ##STR2## wherein R.sub.1 and R.sub.2 are benzyloxy or hydrogen, provided that at least one of R.sub.1 and R.sub.2 is benzyloxy, is subjected to reductive cyclization followed by acetylation of the resultant reaction product.

Abstract: A novel method for the synthesis of 6-hydroxyindolines and new fluorescent dyes produced therefrom, which dyes are ring-constrained indoline-based rhodamine class dyes. These dyes have absorption and emission spectra which make them particularly useful in certain dye laser applications.

Abstract: Indoles of the formula ##STR1## can be prepared by reaction of a phenylhydrazine of the formula ##STR2## which is unsubstituted in at least one ortho-position, with a ketone of the formula ##STR3## in an aqueous medium in the presence of an acid compound, less than 5 equivalents, based on 1 mol of phenylhydrazine, of an acid compound having a pK value of 1.3-4.5 being employed.

Abstract: The invention relates to the use of a 5,6-dihydroxyindoline corresponding to the formula (I): ##STR1## in which R represents a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group, as well as the acid addition salts of these compounds for dyeing keratinous materials, in particular human keratinous materials,and to the tinctorial compositions and methods employed.

Abstract: A process is provided for the preparation of an indole from aniline or a derivative thereof and a polyhydric alcohol. The reaction is carried out in the presence of a catalyst composed of a carrier having a specific surface area of at least 10 m.sup.2 /g and silver supported on the carrier. The catalyst also contains as an additional component a specific amount of at least one element selected from Co, Fe and Ni. Deterioration in catalytic performance of the catalyst during the reaction and its regeneration are therefore minimized.

Abstract: A dehydrocyclization process is described for producing polynuclear organic compounds by contacting a starting organic material having at least one ring moiety comprising at least two adjacent ring carbon atoms each bonded to an independently selected monovalent radical comprising at most about eight carbon atoms provided at least one of the monovalent hydrocarbon radicals comprises more than one carbon atom with a crystalline copper aluminum borate catalyst. The preferred catalyst comprises at least one member selected from the group consisting of (a) crystalline copper aluminum borate and (b) zero valent copper on a support comprising at least one member selected from the group consisting of Al.sub.4 B.sub.2 O.sub.9 and the crystalline copper aluminum borate, the zero valent copper on the support being formed by the reduction of the crystalline copper aluminum borate.

Abstract: Indole derivatives characterized by having a 1,3,4,9-tetrahydropyrano[3,4-b]indole-1-acetic acid nucleus bearing a trifluoromethoxy substituent in the 5-, 6-, 7-, or 8-position, and methods for their preparation and use, are disclosed. The derivatives are useful anti-inflammatory and analgesic agents.

Abstract: A method of synthesizing an indole derivative of the tryptamine type particularly melatonine, comprising the steps of 1) reacting potassium phthalimide and 1,3-di-bromopropane to obtain 3-bromopropylphthalimide; 2) reacting 3-bromopropylphthalimide with sodium acetoacetic ester in ethanol to obtain ethyl-2-acetyl-5-phthalimidopentanoate; 3) reacting the product from step 2) with diazo-p-anisidine to obtain 2-carboxyethyl-3-(2-phthalimidoethyl)-5-methoxy-indole; 4) reacting the 2-carboxyethyl-3-(2-phthalimidoethyl)-5-methoxy-indole with 2N/NaOH and then 20% H.sub.2 SO.sub.4 to obtain impure 5-methoxytriptamine, which is purified by means of hexamethyldisilazane. The mono and disubstituted derivatives are obtained and the monosubstituted derivative is hydrolyzed with aqueous methanol and then recrystallized from ethanol. The N-acetyl derivative is prepared by reaction with acetic anhydride. Melatonine of high purity is obtained for prophylaxy and also against AIDS (Acquired Immuno Deficiency Syndrome).

Abstract: A method for the preparation of 3-(2-aminoethyl)-N-methyl-1H-indole-5-methanesulphonamide by reaction of 4-hydrazino-N-methylbenzenemethanesulphonamide and 4-chloro-1-hydroxybutanesulphonic acid, sodium salt in the presence of an acid.

Abstract: Indole and indole derivatives are prepared by contacting under mild reaction conditions an N-(2-toly)formidate, N-(3-methyl-2-pyridyl)formimidate, or N-methyldiazyl formimidate with an alkali metal amide.

Abstract: A method of preparing indole carboxylic acid derivatives from aniline derivatives is described which can be carried out in a single reaction vessel without any isolation of intermediate products. The method involes reacting an aniline derivative with a soluble nitrite in an acid medium, reducing the resulting nitrosamine by treating the acidic nitrosamine containing reaction solution with zinc in the presence of sufficient acid, optionally with addition of additional acid and/or a solvent such as a lower alcohol, reacting the resulting hydrazine derivative containing solution with a lower alkyl ester of pyruvic acid to obtain a corresponding hydrazone which cyclizes to yield an indole carboxylic acid ester, and if desired, hydrolyzing the ester to obtain the corresponding carboxylic acid.

Abstract: Disclosed herein is to react an aniline and an ethylene glycol at a superatmospheric pressure in preparing an indole by subjecting the aniline and ethylene glycol to a gas-phase catalytic reaction in the presence of a catalyst, thereby improving the selectivity of the reaction and the service life of the catalyst.

Abstract: Disclosed herein is a preparation process for an indole, which process comprises subjecting an N-(.beta.-hydroxy)-alkylaniline, in the presence of a catalyst and at a super-atmospheric pressure, to a gas-phase catalytic reaction. The present process improves the selectivity of the reaction and the service life of the catalyst.

Abstract: A 5-hydroxy-N-substituted indole derivative and the process for producing the indole derivative are described the indole derivative is produced by a process comprising reacting a phenol derivative having an unsaturated double bond in the m-position with a diazonium salt.

Abstract: A method of synthesizing nitrogen heterocycles such as indoles, indolines, oxindoles, quinolines, isoquinolines, and isoquinolones, all of which are pharmacologically active. The method involves cyclizing a haloaryl alkene in the presence of a catalytically effective amount of a palladium(II) ion source and in the presence of a cyclizing promoting base such as an alkali metal salt.

Abstract: A compound of the formula ##STR1## wherein A is the residue of a ACOOH pyrethrinoid acid, Z is selected from the group consisting of hydrogen, --CN, --C.tbd.CH, --CH.sub.3 and alkyl of 1 to 3 carbon atoms, R.sub.1 is selected from the group consisting of hydrogen, alkyl of 1 to 8 carbon atoms, alkenyl and alkynyl of 2 to 8 carbon atoms, cycloalkyl, cycloalkenyl and cycloalkynyl of 3 to 8 carbon atoms, aryl of 6 to 14 carbon atoms and aralkyl of 7 to 18 carbon atoms and R.sub.2 is selected from the group consisting of hydrogen, halogen, alkyl of 1 to 8 carbon atoms, alkenyl and alkynyl of 2 to 8 carbon atoms, cycloalkyl, cycloalkenyl and cycloalkynyl of 3 to 8 carbon atoms, aryl of 6 to 14 carbon atoms, aralkyl of 7 to 18 carbon atoms, --CN, --CF.sub.3, --NO.sub.2 and --COOAlK and AlK is alkyl of 1 to 18 carbon atoms having pesticidal activities.

Abstract: In a process for preparing an indole by reacting an aniline with a diol, a catalyst the activity of which has been reduced through its use in the reaction is brought into contact with an inert gas containing 5 vol. % or less of oxygen so that the catalyst is regenerated for its repeated utilization. The activity of the regenerated catalyst is enhanced further when it is subjected to a reducing treatment for activation upon its reutilization.