In one aspect, the disclosure relates to methods for preparation of intermediates useful for the preparation of aryl-cycloheptene scaffolds. In a further aspect, the disclosed methods pertain to the preparation of compounds comprising an aryl-cycloheptene structure. The disclosed methods utilize abundant starting materials and simple reaction sequences that can be used to modularly and scalably assemble common such cores. In various aspects, the present disclosure pertains to compounds prepared using the disclosed methods. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present disclosure.

The present invention relates to novel manganese complexes and their use, inter alia, for homogeneous catalysis in (1) the preparation of imine by dehydrogenative coupling of an alcohol and amine; (2) CC coupling in Michael addition reaction using nitriles as Michael donors; (3) dehydrogenative coupling of alcohols to give esters and hydrogen gas (4) hydrogenation of esters to form alcohols (including hydrogenation of cyclic esters (lactones) or cyclic di-esters (di-lactones), or polyesters); (5) hydrogenation of amides (including cyclic dipeptides, lactams, diamide, polypeptides and polyamides) to alcohols and amines (or diamine); (6) hydrogenation of organic carbonates (including polycarbonates) to alcohols or hydrogenation of carbamates (including polycarbamates) or urea derivatives to alcohols and amines; (7) dehydrogenation of secondary alcohols to ketones; (8) amidation of esters (i.e., synthesis of amides from esters and amines); (9) acylation of alcohols using esters; (10) coupling of alcohols with water and a base to form carboxylic acids; and (11) preparation of amino acids or their salts by coupling of amino alcohols with water and a hydrogenative coupling of alcohols and amines; (13) preparation of imides from diols.

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The present invention relates to novel manganese complexes and their use, inter alia, for homogeneous catalysis in (1) the preparation of imine by dehydrogenative coupling of an alcohol and amine; (2) CC coupling in Michael addition reaction using nitriles as Michael donors; (3) dehydrogenative coupling of alcohols to give esters and hydrogen gas (4) hydrogenation of esters to form alcohols (including hydrogenation of cyclic esters (lactones) or cyclic di-esters (di-lactones), or polyesters); (5) hydrogenation of amides (including cyclic dipeptides, lactams, diamide, polypeptides and polyamides) to alcohols and amines (or diamine); (6) hydrogenation of organic carbonates (including polycarbonates) to alcohols or hydrogenation of carbamates (including polycarbamates) or urea derivatives to alcohols and amines; (7) dehydrogenation of secondary alcohols to ketones; (8) amidation of esters (i.e., synthesis of amides from esters and amines); (9) acylation of alcohols using esters; (10) coupling of alcohols with water and a base to form carboxylic acids; and (11) preparation of amino acids or their salts by coupling of amino alcohols with water and a hydrogenative coupling of alcohols and amines; (13) preparation of imides from diols.

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Disclosed herein is a method for preparing a 2-arylmalonic acid derivative. In this method, a cyclohexadiene compound is used as a raw material, and sequentially undergoes an isomerization reaction, a halogenation reaction in the presence of a halogenating agent and a dehydrohalogenation-aromatization reaction to obtain a 2-arylmalonic acid derivative (3). An intermediate for preparing the 2-arylmalonic acid derivative (3) and use of the intermediate are also disclosed. ##STR00001##

Disclosed herein is a method for preparing a 2-arylmalonic acid derivative. In this method, a cyclohexadiene compound is used as a raw material, and sequentially undergoes an isomerization reaction, a halogenation reaction in the presence of a halogenating agent and a dehydrohalogenation-aromatization reaction to obtain a 2-arylmalonic acid derivative (3). An intermediate for preparing the 2-arylmalonic acid derivative (3) and use of the intermediate are also disclosed. ##STR00001##

A heavy-atom derivative of CHCA, a primary matrix molecule for matrix-assisted laser desorption/ionization mass spectrometry (MALDI-MS), is synthesized and purified. This new matrix molecule -cyano-4-hydroxy-3-iodocinnamic acid (CHICA) is characterized by .sup.1H NMR and mass spectrometry. CHICA is shown to increase MALDI-MS yield for the test analytes human angiotensin II and sex pheromone inhibitor as compared to both CHCA and an alternative heavy-atom CHCA derivative matrix. An optimal CHICA matrix concentration is determined to be 4 mg/mL. Analyte ion yield is shown to be comparable for CHICA and CHCA for analyte concentrations below 0.001 mg/mL. For analyte concentrations above this threshold, use of CHICA resulted in higher analyte yield and significantly lower relative standard deviation.

A heavy-atom derivative of CHCA, a primary matrix molecule for matrix-assisted laser desorption/ionization mass spectrometry (MALDI-MS), is synthesized and purified. This new matrix molecule -cyano-4-hydroxy-3-iodocinnamic acid (CHICA) is characterized by .sup.1H NMR and mass spectrometry. CHICA is shown to increase MALDI-MS yield for the test analytes human angiotensin II and sex pheromone inhibitor as compared to both CHCA and an alternative heavy-atom CHCA derivative matrix. An optimal CHICA matrix concentration is determined to be 4 mg/mL. Analyte ion yield is shown to be comparable for CHICA and CHCA for analyte concentrations below 0.001 mg/mL. For analyte concentrations above this threshold, use of CHICA resulted in higher analyte yield and significantly lower relative standard deviation.

A stilbene derivative and a method of preparing the A stilbene derivative are disclosed. The stilbene derivative is provided for inhibiting the function of cyclophilin, which is effective at the prevention of cyclophilin-related diseases or at the treatment of symptoms of such diseases. The method of preparing a stilbene derivative includes reacting a phenylacetonitrile derivative with a benzaldehyde derivative.

This invention relates to a stilbene derivative and a method of preparing the same, and more particularly to a novel stilbene derivative for inhibiting the function of cyclophilin, which is effective at the prevention of cyclophilin-related diseases or at the treatment of symptoms of such diseases, and to a method of preparing the same.

A heavy-atom derivative of CHCA, a primary matrix molecule for matrix-assisted laser desorption/ionization mass spectrometry (MALDI-MS), is synthesized and purified. This new matrix molecule -cyano-4-hydroxy-3-iodocinnamic acid (CHICA) is characterized by .sup.1H NMR and mass spectrometry. CHICA is shown to increase MALDI-MS yield for the test analytes human angiotensin II and sex pheromone inhibitor as compared to both CHCA and an alternative heavy-atom CHCA derivative matrix. An optimal CHICA matrix concentration is determined to be 4 mg/mL. Analyte ion yield is shown to be comparable for CHICA and CHCA for analyte concentrations below 0.001 mg/mL. For analyte concentrations above this threshold, use of CHICA resulted in higher analyte yield and significantly lower relative standard deviation.