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Cu-catalyzed oxidative amidation of propiolic acids under air via decarboxylative coupling

Figure presented A Cu-catalyzed aerobic oxidative amidation of propiolic acids via decarboxylation under air has been developed. Only carbon dioxide is produced as byproduct in this approach. The use of air as oxidant makes this method more useful and easy to handle.

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A METHOD FOR THE PREPARATION OF ZOLMITRIPTAN

In the preparation of zolmitriptan of formula III the reduction of the diazonium salt to (5)-4-(4- hydrazinobenzyl)-l,3-oxazolidin-2-one of formula IV is performed in a more concentrated mixture and by the effect on an alkali metal disulphite, preferably sodium disulphite. A zolmitriptan toluene solvate, characterized by a toluene content of 9 to 14 % by weight according to the gas chromatography determination and by a maximum of the corresponding mass loss at temperatures of about 111C in the gravimetric analysis record. A zolmitriptan toluene solvate, showing strong Raman bands at the wave numbers of 1443 and 1354 cm-1, characteristic for the crystal lattice of zolmitriptan with built-in toluene, and further marked bands at 1004 and 786 cm-1, characteristic for toluene.

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Conversion of Ester Moieties to 4-Bromophenyl Groups via Electrocyclic Reaction of Dibromocyclopropanes

(Chemical Equation Presented) Conversion of ester moieties into 4-bromophenyl groups was effected by means of a four-step protocol: a Grignard reaction of the ester with allylmagnesium halides, a ring-closing metathesis, dibromocyclopropanation, and an electrocyclic reaction of the dibromocyclopropanes.

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Solution and solid state studies of hydrogen bonding in substituted oxazolidinones by spectroscopic and quantum chemical methods

Structure and hydrogen bonding interactions of bioactive oxazolidinones have been studied by means of NMR and vibrational spectroscopies and quantum chemical calculations. We have demonstrated that oxazolidinone derivatives form hydrogen bonds in solution and solid state. Conformational space search has revealed predominant conformations in solution. In low polarity solvents, such as chloroform, dimers are formed presumably by intermolecular hydrogen bonds between two oxazolidinone molecules forming the most stable complexes, which has also been found in the solid state by IR spectroscopy and crystallography. In solvents of higher polarities, like methanol and dimethylsulfoxide, intermolecular interactions with solvent molecules and in dimers are present. As expected, raising the temperature broke hydrogen bonds, which was reflected in down-field chemical shifts of corresponding resonances. On the other hand, raising the solution concentration considerably affected oxazolidinone resonances only in chloroform, corroborating the formation of oxazolidinone dimers. These results may help in better understanding oxazolidinone structure, properties and interactions when designing new bioactive compounds and pharmaceutical products.

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In homogeneous catalysis, the catalyst is in the same phase as the reactant. The number of collisions between reactants and catalyst is at a maximum.In a patent, 3190-70-3, name is (S)-4-Isobutyloxazolidine-2,5-dione, introducing its new discovery. Formula: C7H11NO3

Urethane-protected amino acid-N-carboxyanhydrides

Urethane-protected NCAs and MTAs are prepared by reacting an NCA or NTA with a haloformate in an inert diluent, under anhydrous conditions and in the presence of a tertiary nitrogen-containing base having an atom or functional group sufficiently electron rich and positioned relative to the nitrogen of said base so as to render said atom or group capable of complexing with the H–N< group of said N-carboxyanhydride or N-thiocarboxyanhydride but able to generate N-carboxyanhydride or N-thiocarboxyanhydride anionic complexes capable of reacting with the haloformate. We¡¯ll also look at important developments in the pharmaceutical industry because understanding organic chemistry is important in understanding health, medicine, the role of 3190-70-3, and how the biochemistry of the body works.Formula: C7H11NO3

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Iron-catalyzed amidation of alkynyl bromides: A facile route for the preparation of ynamides

(Chemical Equation Presented) A facile route to obtain ynamides in high yields was described. The products were achieved through the iron-catalyzed C-N coupling reaction of amides with alkynyl bromides in the presence of 20 mol % of N,N?-dimethylethane-1,2-diamine (DMEDA).

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Pyran-2-ones and 5,6-dihydropyran-2-ones useful for treating hyperplasia and other diseases

Certain 2H-pyran-2-ones are useful for treating benign prostatic hypertrophy or hyperplasia, prostatic cancer, alopecia, hirsutism, acne vulgaris and seborrhea.

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MIGRASTATIN ANALOGS IN THE TREATMENT OF CANCER

In one aspect, the present invention provides a method for treating colon and/or ovarian cancer in a subject comprising administering to a subject in need thereof a compound of general formula (I): wherein R1-R6, R, ,-R,, Q, Y1, Y2 and n are as defined herein, wherein the compound is present in an amount effective to inhibit colon and/or ovarian tumor metastasis.

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N-BENZYL OXAZOLIDINONES AND RELATED HETEROCYCLEIC COMPOUNDS AS POTENTIATORS OF GLUTAMATE RECEPTORS

Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula (I) as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed. The compounds are active as potentiators of glutamate receptors, in particular mGluR2.

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PROCESS FOR PREPARING POSACONAZOLE AND INTERMEDIATES THEREOF

The present invention relates to an industrially advantageous process for the preparation of tetrahydrofuran antifungals preferably posaconazole of formula I. The present invention further relates to improved processes for preparing key and novel intermediates useful in the preparation of posaconazole. The present invention further relates to improved processes for preparing the compound of formula II, a key intermediate in the preparation of posaconazole.

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