Abstract:
A process for preparing a substituted aromatic compound, comprising combining an aromatic compound and cuprous (Cu+) ions in a reaction vessel in an essentially oxygen-free environment, and adding to said reaction vessel a source of an electrophile or a nucleophile substituent, to form an aromatic compound product which is ring-substituted with said electrophile or nucleophile at a position which was originally occupied by hydrogen, and isolating the substituted aromatic compound from the reaction mixture.
Abstract:
The present invention discloses a process for efficient production of 2-amino-5- hydroxypropiophenone corresponding to the AB ring part of camptothecin (CPT) skelton, which is a key intermediate useful for the total synthesis of camptothecin analogs including 7-Ethyl-10-hydroxy camptothecin and novel intermediates thereof.
Abstract:
The present invention relates to a novel process for the preparation of compounds of Formula (I) wherein X, Q, R 1 and R 2 are as defined in the specification, the compounds being useful in the preparation of therapeutic agents. The invention further relates to novel intermediates useful in the preparation of the therapeutic agents.
Abstract:
A process for producing a bis(4-hydroxy-3-nitrophenyl) compound, characterized in that a bis(4-hydroxyphenyl) compound comprising two phenyl groups bonded to each other directly or through an electron-donating bridging group, sulfoxide group, sulfone group, or carbonyl group is nitrated with nitric acid in an inert solvent substantially in the absence of any other acid. By the process, the target compound reduced in the content of trinitro-substituted compounds can be produced in high yield. Recrystallizing the compound easily gives in high yield a high-purity product suitable for use as a raw material for a heat-resistant polymer, etc., because the content of trinitro-substituted compounds in that compound is low.
Abstract:
Disclosed herein is an improvement in a method for making compounds having the structural formulae (I) or (II) wherein: X is a) phenyl; lower phenylalkoxy, phenoxy; or benzyl; or b) one subtituent from group a) and one or more substituents selected from C1-C4 alkoxy; hydroxyl; halogen; lower alkyl; and lower alkylthio; or c) along with the phenyl to which it is attached, forms a multiple fused ring heterocycle such as dibenzofuranyl; Y is H, C1-C4 alkanoyl, C1-C4 haloalkanoyl, dialkoxyphosphoryl, alkylaminocarbonyl, haloalkylsulfonyl, or C1-C4 alkoxy carbonyl; and R is H, C1-C6 alkyl, C1-C6 alkoxy, C3-C6 cycloalkoxy, haloalkyl, alkoxyalkyl, arylalkoxy, alkenyl, alkylthio, alkoxycarbonyl, alkylamino, heteroaryl, arylalkyl, haloalkoxy, aryloxy, or C3-C6 cycloalkyl; and Z is O or S, wherein the improvement comprises the steps of: A) selecting as a starting material a compound of structural formula (III); B) dissolving compound III in an organic solvent selected from the group consisting of methyl t-butyl ether, ethylene glycol dimethyl ether, 2-methoxyethyl ether, acetonitrile, and acetic acid, and C) nitrating with nitric acid to form a compound of structural formula (IV).
Abstract:
The subject invention involves processes for making 2,4-difluoro-3-Q1-benzoic acid, wherein Q1 is derived from an electrophilic reagent, comprising the steps of: (a) treating 1-bromo-2,4-difluorobenzene with a strong, non-nucleophilic base; then treating with an electrophilic reagent which provides Q1, or a functional moiety which is then transformed to Q1, producing 1-bromo-2,4-difluoro-3-Q1-benzene; (b) treating the 1-bromo-2,4-difluoro-3-Q1-benzene with an alkali or alkaline earth metal or organometallic reagent; then treating with carbon dioxide, or with a formylating agent followed by oxidation, to produce 2,4-difluoro-3-Q1-benzoic acid. The subject invention also involves optional additional steps to further modify Q1, or to substitute a non-hydrogen moiety at the 5-position, at the 6-position, or at both, of the phenyl ring of the 2,4-difluoro-3-Q1-benzoic acid.
Abstract:
A solvent free process for the nitration of an aromatic compound using an aluminosilicate catalyst which has been treated with nitric acid and an acid anhydride. The process enables nitrated aromatic compounds to be produced in high yields and with good regioselectivity. The process also avoids the need to recover the nitrated product from large volumes of solvent and avoids treatment of inorganic acid waste, both of which may be undesirable for environmental reasons.
Abstract:
Porous microcomposites have been prepared from perfluorinated ion-exchange polymer and metal oxides such as silica using the sol-gel process. Such microcomposites possess high surface area and are useful as catalysts for olefin isomerization.
Abstract:
The present invention provides an acid catalyst complex comprising an organosulfonic acid having at least one covalent carbon-fluorine bond or one covalent carbon-phosphorus bond provided by a phosphono radical which has been contacted with a Lewis Acid to produce a catalyst complex containing said Lewis Acid. The present invention also provides a process for the conversion of a reactant into a reaction product in the presence of said catalyst complex. In particular, the catalyst complex is useful for providing a high octane alkylate stream by converting a mixture comprising isoparaffins and olefins into said alkylate in the presence of said catalyst complex.
Abstract:
Described is a method of preparing 5-alkoxy-2,4-dinitroalkylbenzene compounds of general formula (I), in which R1 is C1-C4 alkyl and R is C1-C6 alkyl, C2-C4 hydroxyalkyl or C3-C4 dihydroxyalkyl. The method calls for a 3-fluoroalkylbenzene to be nitrated and the 2,4-dinitro-5-fluoroalkylbenzene thus obtained to be reacted, after addition of sodium hydroxide or potassium hydroxide, with a suitable alcohol at -5 to +25 °C.