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PROCESS FOR THE PREPARATION OF ZIPRASIDONE (5-[2-[4-(1,2-BENZISOTHIAZOL-3-Y1)-1-PIPERAZINY1]ETHY1]-6-CHLORO-1,3-DIHYDRO-2H-INDOL-2-ONE)

The present invention provides a new and useful process for preparing 5-[2-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]ethyl]-6-chloro-1,3?dihydro-2H-indol-2-one (ziprasidone) and methods for its purification. The process comprises the steps of: (i) mixing 6-chloro-5-(2-chloroethyl)-1,3-dihydro-2H-indol-2-one with either a free base or salt form of 3-(1-piperazinyl)-1,2?benzoisothiazole, in the presence of an alkaline compound and a high-boiling polar organic solvent or mixture of high boiling polar organic solvents, (ii) heating the mixture and stirring for a sufficient amount of time to obtain ziprasidone formation, (iii) cooling the mixture, adding it to water and filtering off the product, (iv) adding water to the product and stirring the suspension, and (v) isolating crude ziprasidone.

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87691-88-1, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.87691-88-1, Name is 3-Piperazinobenzisothiazole hydrochloride, molecular formula is C11H14ClN3S. In a Article, authors is Sharma£¬once mentioned of 87691-88-1

Novel urea and thiourea derivatives of thiazole-glutamic acid conjugate as potential inhibitors of microbes and fungi

Since discovery and development of effective as well as safe drugs has brought a progressive era in human healthcare that is accompanied by the appearance of drug resistant bacterial strains, there is constant need of new antibacterial agent having novel mechanisms of action to act against the harmful pathogens. In the present study, several N-terminal substituted urea/thiourea derivatives were synthesized by the reaction of glutamic acid and 3-(1-piperazinyl)-1,2-benzisothiazole with various substituted phenyl isocyanates/isothiocyanates. Elemental analysis, IR, 1H NMR, 13C NMR and mass spectral data confirmed the structure of the newly synthesized compounds. The derivatives were investigated for their antibacterial and antifungal activities against various pathogens of human origin by agar well diffusion method and microdilution method. The preliminary antimicrobial bioassay reveals that the compounds containing fluoro and bromo as substituents showed promising antimicrobial activity. Pleiades Publishing, Ltd., 2013.

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A and Cefotetan disodium method for the preparation of intermediates (by machine translation)

The invention discloses a Cefotetan disodium method for the preparation of intermediates thereof, the commercial raw material 4 – (1-amino-3-tert-butoxy -1,3-dioxo-2-ene yl) – 1,3-dithio-azetidine-2-carboxylic acid (2) and 7-MAC (3) for a condensation reaction to make compound 4, after deprotection, salification Cefotetan disodium (1). The invention also provides the compound 2 preparation method. The conventional route of the route to avoid pollution of the environment of the use of chloride reagent, with simple process route, process cost reduction, the overall yield of product is improved, friendly characteristic of the environment, is suitable for industrial production. (by machine translation)

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N-SUBSTITUTED PIPERIDINE AND PIPERAZINE DERIVATIVES

This invention relates to compounds of the formula 1 wherein R1, R2, R7, R8, R9, U, V, Z, A, W, X, M, E, L, T and D are defined as in the specification, pharmaceutical compositions containing them and their use in the treatment of central nervous system and other disorders.

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Isothiazole – Wikipedia,
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Chemistry is the experimental and theoretical study of materials on their properties at both the macroscopic and microscopic levels.In a patent£¬Which mentioned a new discovery about 107869-45-4, molcular formula is C10H15NO2S, introducing its new discovery. , 107869-45-4

Process for the preparation of substituted pyrrolidine derivatives and intermediates

Two syntheses are provided; one for the preparation of (3R,4R)-4-(hydroxymethyl)pyrrolidin-3-ol, and other for the preparation of (3S,4R)-4-(hydroxymethyl)pyrrolidin-3-ol. (3R,4R)-4-(hydroxymethyl)pyrrolidin-3-ol is prepared using the achiral ylide prepared from benzylamine instead of phenethylamine (Scheme 3) which provides a crystalline intermediate. The synthesis of (3S,4R)-4-(hydroxymethyl)pyrrolidin-3-ol is achieved from (S)-diethylmalate as described in Scheme 4. A process for preparing camphor sultam is also provided.

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Isothiazole – Wikipedia,
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677304-78-8, 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, 677304-78-8, name is 5-Bromobenzo[d]isothiazole-3-carboxylic acid, introducing its new discovery.

N-HETEROARYL COMPOUNDS WITH CYCLIC BRIDGING UNIT FOR THE TREATMENT OF PARASITIC DISEASES

This invention relates to certain N-heteroaryl compounds that are generally useful as medicaments, more specifically as medicaments for animals. The medicament can preferably be used for the treatment of helminth infections and the treatment of parasitosis, such as caused by helminth infections. This invention also relates to uses of the compounds to make medicaments and treatments comprising the administration of the compounds to animals in need of the treatments. This invention also relates to the preparation of the N-heteroaryl compounds. Moreover this invention relates to pharmaceutical compositions and kits comprising the compounds.

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677304-78-8, Chemistry is the experimental science by definition. We want to make observations to prove hypothesis. For this purpose, we perform experiments in the lab. 677304-78-8, Name is 5-Bromobenzo[d]isothiazole-3-carboxylic acid,introducing its new discovery.

Novel Annelation Method to Pyridine and Isoquinoline by Photochemical Means

Intramolecular photoaddition reactions of 2-(omega-alkenyl)isoquinolin-1(2H)-ones and 1-(omega-alkenyl)pyridin-2(1H)-ones were examined, and the regioselectivity and dependence of these reactions on the length of methylene chain in the alkenyl group were clarified.By utilizing these reactions, a synthetic route to indolizine and quinolizine derivates was elaborated.By an extension of this approach to the intermolecular reaction, 6-methoxy-3-methyl-1,2-dihydrocyclobutapyridin-4(3H)-one was synthesized from 4,6-dimethoxy-1-methylpyridin-2(1H)-one.Keywords-2+2 photocycloaddition; intramolecular photoaddition; photocycloreversion; annelation; indolizine; quinolizine; cyclobutapyridine; 4,6-dimethoxypyridin-2(1H)-one; 1-(omega-alkenyl)pyridin-2(1H)-one; 2-(omega-alkenyl)isoquinolin-1(2H)-one

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Isothiazole – Wikipedia,
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107869-45-4, Chemistry can be defined as the study of matter and the changes it undergoes. You¡¯ll sometimes hear it called the central science because it is the connection between physics and all the other sciences, starting with biology.107869-45-4, Name is (3aR,6S)-8,8-Dimethyl-4,5,6,7-tetrahydro-3H-3a,6-methanobenzo[c]isothiazole 2,2-dioxide, molecular formula is C10H15NO2S, introducing its new discovery.

Progress toward the total synthesis of callipeltin A (I): Asymmetric synthesis of (3S,4R)-3,4-dimethylglutamine

(equation presented) During the total synthesis of the novel cyclic depsipeptide callipeltin A (1), the unit (3S,4R)-3,4-dimethylglutamine, was successfully synthesized by asymmetric Michael addition and subsequent electrophilic azidation. The key feature of this approach is the generation of three adjacent stereogenic centers using the same camphorsultam chiral auxiliary.

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The important role of (3aR,6S)-8,8-Dimethyl-4,5,6,7-tetrahydro-3H-3a,6-methanobenzo[c]isothiazole 2,2-dioxide

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107869-45-4, An article , which mentions 107869-45-4, molecular formula is C10H15NO2S. The compound – (3aR,6S)-8,8-Dimethyl-4,5,6,7-tetrahydro-3H-3a,6-methanobenzo[c]isothiazole 2,2-dioxide played an important role in people’s production and life.

Asymmetric synthesis of sultams and sulfonamides via diastereoselective reduction of N-sulfonylimines

The diastereoselective reduction of both cyclic and acyclic camphor sulfonylimines was investigated. With cyclic camphor sulfonylimines 1, reduction using NaBH4 in methanol afforded the corresponding camphorsultams 2 in 92-95% yield as single diastereomers with the exception of 1c where debromination occurred prior to reduction. For the large scale preparation of camphorsultam 1a and its derivatives, important chiral auxiliaries in asymmetric synthesis, reduction with NaBH4 is the reagent of choice. Reduction of acyclic camphor sulfonylimines 7 to camphorsulfonamides 8 with the bulky reducing reagent, LiAl(OBu-i)3H afforded the highest de’s (>90% de) and yields 90-95%.

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A PROCESS FOR THE PREPARATION OF OXINDOLE DERIVATIVES

A process for the preparation of oxindole derivative of formula (I) comprising reacting compound of formula (II) with dialkyl malonate, COOR1-COOR1, in the presence of a mild base to give compound of formula (III); and wherein R is selected from hydrogen, linear, branched or cyclic alkyl, aryl, substituted aryl, heteroaryl, haloalkyl like CF3, alkoxy, haloalkoxy, thioalkyl and halogen.; R1 is selected from linear, branched and cyclic alkyl (C1 to C4 groups); and X is selected from chloro, bromo, fluoro and iodo groups;further converting compound of formula (III) to compound of formula (I).

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