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Scale gear heterocyclic derivatives and their application in the multi-target anti- depression (by machine translation)

The invention discloses a scale gear heterocyclic compound or its pharmaceutically acceptable salt, has the following structure, The compounds and compositions containing the same to the 5 – HT reuptake, 5 – HT1 A Receptor and 5 – HT7 Receptor has activity, it can be applied to the preparation of novel anti-depression drug. (by machine translation)

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PROCESS FOR PREPARING ZIPRASIDONE

The present invention concerns a process for the preparation of 5-(2-(4-(1,2- 5 benzisothiazol-3-yl)-1-piperazinyl)ethyl)-6-chloro-1,3-dihydro-2H-indol-2-one of the formula (I), or a pharmaceutically acceptable acid addition salt, solvate, hydrates or clathrate thereof, said process comprising reacting a compound of formula (II) wherein X is a halogen atom, with a compound of formula (III), said compound of formula (III) being the free base or an addition salt with an organic or inorganic acid, wherein said process is characterized in that said compounds according to formulas (II) and (III) are reacted in the presence of a neutralizing agent, and are reacted in a solvent comprising acetonitrile.

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The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.SDS of cas: 677304-75-5, Name is 6-Bromobenzo[d]isothiazole-3-carboxylic acid, molecular formula is C8H4BrNO2S, SDS of cas: 677304-75-5. In a Patent, authors is £¬once mentioned of SDS of cas: 677304-75-5

COMPOUNDS AND METHODS FOR MODULATING FXR

Compounds of formula (I): formula (I) wherein variables are as defined herein and their pharmaceutical compositions and methods of use are disclosed as useful for treating dyslipidemia and diseases related to dyslipidemia.

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We¡¯ll also look at important developments in the pharmaceutical industry because understanding organic chemistry is important in understanding health, medicine, the role of 677304-75-5, and how the biochemistry of the body works.HPLC of Formula: C8H4BrNO2S

Chemistry is the science of change. But why do chemical reactions take place? Why do chemicals react with each other? The answer is in thermodynamics and kinetics.In a document type is Patent, the author is and a compound is mentioned, HPLC of Formula: C8H4BrNO2S, 6-Bromobenzo[d]isothiazole-3-carboxylic acid, introducing its new discovery. HPLC of Formula: C8H4BrNO2S

COMPOUNDS AND METHODS FOR MODULATING FXR

Compounds of formula. wherein variables are as defined herein and their pharmaceutical compositions and methods of use are disclosed as useful for treating dyslipidemia and related diseases.

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Benzisothiazole and benzisoxazole piperazine derivatives

Disubstituted N,N-piperazinyl derivatives are disclosed wherein one substituent is benzisothiazol-3-yl or benzisoxazol-3-yl and the other is alkylene attached to heterocycles such as azaspiro[4.5]decanedione, dialkylglutarimide, thiazolidinedione and spirocyclopentylthiazolidinedione or butyrophenone-like groups. The compounds have psychotropic properties and 8-[4-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]butyl]-8-azaspior[4.5]decane-7,9-dione is a typical embodiment having selective antipsychotic activity.

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A process for the preparation of intermediates […] (by machine translation)

The invention relates to a process for the preparation of intermediates […], the intermediate body is (3aR, 7aR) – 4 ? – (1,2-benzisothiazol-3-yl) eight hydrogen spiral [2H-isoindole -2,1 ?-piperazine] a sulfonate. The (1R, 2R) – 1,2-cyclohexane dimethanol as raw materials, dialkyltinacetal after armor is a sulfonic acid ester, with the 3 – (1-piperazinyl) – 1,2 benzothiazin hydrochloride reaction to obtain the required intermediate. (by machine translation)

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Chemistry of Oxaziridines. 18. Synthesis and Enantioselective Oxidations of the <(8,8-Dihalocamphoryl)sulfonyl>oxaziridines

The synthesis and enantioselective oxidations of <(8,8-dihalocamphoryl)sulfonyl>oxaziridines 13 are reported.These reagents are prepared in two steps from the (camphorylsulfonyl)imine 4 by treatment of the corresponding azaenolate with electrophilic halogen sources followed by biphasic oxidation of the resulting dihalo imine 6-9 with m-CPBA/K2CO3.Of these oxaziridines the dichloro reagent 13b, available on a multigram scale, affords the highest enantioselectivities for the asymmetric oxidation of sulfides to sulfoxides (42-74 percent) and for the hydroxylation of enolates (often better than 95 percent ee).In general the molecular recognition is predicted and explained in terms of minimization of nonbonded steric interactions in the transition states.For the asymmetric oxidation of sulfides to sulfoxides, secondary electronic factors related to the polarity of the sulfide and oxaziridine also play a role.Definitive evidence for chelation of the metal enolate with the C-X bond in 13 is not found.The molecular recognition is interpreted in terms of the higher reactivity of the reagents and an active-site structure which is sterically complementary with the enolate.For the asymmetric hydroxylation of the Z- and E-enolates of propiophenone (16a), the Z-enolate exhibits much higher stereoselectivity than the E-enolate: >95 percent vs 22 percent ee.

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PHENYLALKYL AND PYRIDYLALKYL PIPERAZINE DERIVATIVES

This invention relates to compounds of the formula (1) wherein R1, R3, R4, X1 , and X2 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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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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Continuation of structure?activity relationship study of novel benzamide derivatives as potential antipsychotics

A series of benzamide derivatives possessing potent dopamine D2, serotonin 5-HT1A, and 5-HT2A receptor properties were synthesized and evaluated as potential antipsychotics. Among them, 5-(4-(4-(benzo[d]isothiazol-3-yl)piperazin-1-yl)butoxy)-N-cyclopropyl-2-fluorobenzamide (4k) held the best pharmacological profile. It not only exhibited potent and balanced activities for the D2, 5-HT1A, and 5-HT2A receptors, but was also endowed with low to moderate activities for the 5-HT2C, H1, and M3 receptors, suggesting a low propensity for inducing weight gain or diabetes. In animal models, compound 4k reduced phencyclidine-induced hyperactivity with a high threshold for catalepsy or muscle relaxation induction. On the basis of its robust in vitro potency and in vivo efficacy in preclinical models of schizophrenia, 4k was selected as a candidate for further development.

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