cas 16263-52-8, 3-Chloro-1,2-benzisoxazole

Articles about 16263-52-8Total 6 be found

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An efficient synthesis of oxazolines: Via a cascade reaction between azaoxyallyl cations and 1,2-benzisoxazoles
A formal [3 + 2] cycloaddition reaction between the C and O terminals of azaoxyallyl cations formed in situ and 1,2-benzisoxazoles has been realized. This one-pot cycloaddition method provided an effective and practical pathway to synthesize oxazoline in good yields under mild conditions. The title products exhibited unique fluorescence properties.
Sun, Li,Liu, Yi,Wang, Yankai,Li, Yuanyuan,Liu, Zhiwen,Lu, Tao,Li, Wenhai
supporting information
p. 7526 - 7530
(2019/08/20)

Synthesis of a bicyclic piperazine from l-aspartic acid and application of a fluoride-promoted SNAr coupling
The process development is reported of a pivotal C-N bond formation involving ((7R,9aS)-octahydro-1H-pyrido[1,2-a]pyrazin-7-yl)methanol (2) undergoing nucleophilic aromatic substitution with 3-chlorobenzo[d]isoxazole (3) to furnish ((7R,9aS)-2-(benzo[d]isoxazol-3-yl)octahydro-1H-pyrido[1,2-a] pyrazin-7-yl)methanol (4) as a key intermediate for a family of compounds (1). Essential to the success of the coupling is the use of fluoride in combination with a phase transfer catalyst. The development of an alternative route to bicyclic piperazine 2 that uses l-aspartic acid (20) as a starting material to avoid the need for a classical salt resolution is described.
Sieser, Janice E.,Singer, Robert A.,McKinley, Jason D.,Bourassa, Dennis E.,Teixeira, John J.,Long, James
experimental part
p. 1328 - 1335
(2012/01/12)

PROLINE DERIVATIVES AND USE THEREOF AS DRUGS
The present invention aims at providing compounds having therapeutic effects due to a DPP-IV inhibitory action, and satisfactory as pharmaceutical products. The present inventors have found that derivatives having a substituent introduced into the γ-position of proline represented by the formula (I) wherein each symbol is as defined in the specification, have a potent DPP-IV inhibitory activity, and completed the present invention by increasing the stability.
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(2008/06/13)

Synthesis of an Optically Active Octahydro-2H-pyridopyrazine Based CNS Agent
A synthesis of an optically active octahydro-2H-pyridopyrazine is presented.The key sequence involved the equilibration of an optically active cis-aldehyde to give the thermodynamic transaldehyde that was trapped by nitromethane anion.
Urban, Frank J.,Breitenbach, Ralph,Murtiashaw, Charles W.,Vanderplas, Brian C.
p. 321 - 324
(2007/10/02)

Synthesis and Biological Evaluation of 1-(1,2-Benzisothiazol-3-yl)- and (1,2-Benzisoxazol-3-yl)piperazine Derivatives as Potential Antipsychotic Agents
Members of the series of title compounds were tested for potential antipsychotic activity in relevant receptor binding assays and behavioral screens.Structure-activity relationships within the series are discussed.Compound 24 (BMY 13859-1), a (1,2-benzisothiazol-3-yl)piperazine derivative, was selected for further study because of its potent and selective profile in primary CNS tests.It was active in the Sidman avoidance paradigm and blocked amphetamine-induced stereotyped behavior in dogs for up to 7 h.The compound's lack of typical neuroleptic-like effects in therat catalepsy test and its failure to produce dopamine receptor supersensitivity following chronic administration indicate that it should not cause the movement disorders commonly associated with antipsychotic therapy.Although 24 has potent affinity for dopaminergic binding sites, its even greater affinity for serotonin receptors suggests that a serotonergic component may be relevant to its atypical profile.Compound 24 is currently undergoing clinical evaluation in schizophrenic patients.
Yevich, Joseph P.,New, James S.,Smith, David W.,Lobeck, Walter G.,Catt, John D.,et al.
p. 359 - 369
(2007/10/02)

Biological properties of 1,2 benzisothiazoles compounds. Local anesthetic activity of 3,alkylaminoalkoxybenzisothiazoles
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Vitali,Mossini,Bertaccini,Impicciatore
p. 1081 - 1096
(2007/10/04)

Chemical Properties

Melting Point: 31 °C
Boiling Point: 251.206 °C at 760 mmHg
Flash Point:105.726 °C
Density: 1.377 g/cm³
Storage Temp.:under inert gas (nitrogen or Argon) at 2-8°C
Vapor Pressure: 0.033mmHg at 25°C
Refractive Index: 1.624
PKA: -5.47±0.30(Predicted)
PSA: 26.03000
LogP: 2.48120

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16263-52-8

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Chemical Properties

Melting Point: 31 °C

Boiling Point: 251.206 °C at 760 mmHg

Flash Point:105.726 °C

Density: 1.377 g/cm³

Storage Temp.:under inert gas (nitrogen or Argon) at 2-8°C

Vapor Pressure: 0.033mmHg at 25°C

Refractive Index: 1.624

PKA: -5.47±0.30(Predicted)

PSA: 26.03000

LogP: 2.48120

Global suppliers and manufacturers of 16263-52-8total 53 suppliers on LookChem

Article Database

16263-52-8

Articles about 16263-52-8Total 6 be found

More Articles about upstream products of 16263-52-8

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Chemical Properties

Melting Point: 31 °C

Boiling Point: 251.206 °C at 760 mmHg

Flash Point:105.726 °C

Density: 1.377 g/cm3

Storage Temp.:under inert gas (nitrogen or Argon) at 2-8°C

Vapor Pressure: 0.033mmHg at 25°C

Refractive Index: 1.624

PKA: -5.47±0.30(Predicted)

PSA: 26.03000

LogP: 2.48120

Global suppliers and manufacturers of 16263-52-8total 53 suppliers on LookChem

Density: 1.377 g/cm³