Category: 87691-88-1

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Method for preparing Perospirone is (by machine translation)

The invention discloses a new method for preparing Perospirone is of the, type I and along link oneself dimethyl ester imide reaction, produce Perospirone is, the method avoids the alkylation intermediate, has the advantages of simple process, raw materials are easy, is suitable for industrial production, the product yield and purity are, and the like. (by machine translation)

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Reference£º
Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com

 

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3-[4-(1-Substituted-4-piperazinyl)butyl]-4-thiazolidinone compounds

3-[4-1-substituted-4-piperazinyl)butyl]-4-thiazolidinone compounds which are useful as antipsychotic, analgesic, anticonvulsant and anxiolytic agents.

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Isothiazole – Wikipedia,
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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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Reference£º
Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com

 

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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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Isothiazole – Wikipedia,
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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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Isothiazole – Wikipedia,
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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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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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Isothiazole – Wikipedia,
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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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Isothiazole – Wikipedia,
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In heterogeneous catalysis, the catalyst is in a different phase from the reactants. Quality Control of 3-Piperazinobenzisothiazole hydrochloride, At least one of the reactants interacts with the solid surface in a physical process called adsorption in such a way. 87691-88-1, name is 3-Piperazinobenzisothiazole hydrochloride. In an article£¬Which mentioned a new discovery about 87691-88-1

New disulfide route to 3-(1-piperazinyl)-1,2-benzisothiazole. Nucleus for atypical antipsychotic drugs

A new, one-step commercial process for the preparation of 3-(1-piperazinyl)-l,2-benzisothiazole hydrochloride, a key intermediate for the syntheses of some new, “atypical antipsychotic” drugs, was developed. Reaction of bis(2-cyanophenyl) disulfide with excess piperazine at 120-140 C for 3-24 h in the presence of small amounts of DMSO and 2-propanol formed 3-(l-piperazinyl)-l,2-benzisothiazole in 75-80% yields. The DMSO oxidized the liberated 2-mercaptobenzonitrile to regenerate bis(2-cyanophenyl) disulfide, thereby enabling the utilization of both halves of the symmetrical disulfide to generate product. The reaction mechanism for the conversion of the bis(2-cyanophenyl) disulfide to 3-amino-1,2-benzisothiazole involves the formation of ring-opened sulfenamide and benzamidine intermediates and then their subsequent ring closure to regenerate the 1,2-benzisothiazole nucleus. A safe, efficient, and robust process to prepare 3-(l-piperazinyl)-1,2-benzisothiazole under very concentrated reaction conditions was developed and successfully scaled up in the pilot plant to support the development of ziprasidone.

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Reference£º
Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com

 

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CONDENSED THIOPHENE COMPOUND AND PHARMACEUTICAL USE THEREOF

A condensed thiophene compound represented by general formula: STR1 or a pharmaceutically acceptable salt thereof, wherein ring S represents a thiophene ring; R 1 represents hydrogen, halogen, alkyl, etc.; R 2 represents hydrogen, alkyl, acyl, etc.; G represents–CH. sub.2–,–CH(OH)–,–CO–, etc.; Q represents alkylene; T represents–N(Rb)(Rc) (wherein Rb, Rc represents each alkyl etc.; or alternatively Rb and Rc are combined together to form cyclic amino); D represents–CH. sub. 2–or–S–; A and B represent each carbonyl or thiocarbonyl, or are null; and m and n represent each 0, 1 to 4, provided that m+n represents an integer of 4 or less.

This compound is useful as an antipsychotic drug having a reduced extrapyramidal side effect.

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Reference£º
Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com