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Lactam derivative and application thereof

A compound, halogen technology, applied in the field of medicine, can solve problems such as QT interval prolongation

Inactive Publication Date: 2017-05-31
NHWA PHARMA CORPORATION
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the atypical antischizophrenic drugs currently in clinical use all have adverse reactions such as QT interval prolongation and high prolactin to varying degrees]

Method used

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  • Lactam derivative and application thereof
  • Lactam derivative and application thereof
  • Lactam derivative and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0094] Example 1, 7-(4-(4-(6-fluorobenzo[d]isoxazol-3-yl)piperidinyl-1-yl)butoxy)-2-methyl-3,4 -Dihydroisoquinolin-1(2H)-one (1)

[0095](1) 4-Methoxyphenethylamine (0.1mol) was dissolved in 300ml of dichloromethane, cooled to 0°C in an ice bath, 20ml of triethylamine was added, and ethyl chloroformate (0.15mmol) was slowly added dropwise thereto , After adding, react at room temperature for 12h. After the reaction was completed, the reaction solution was washed with water and 10% dilute hydrochloric acid solution, the organic layer was dried with anhydrous magnesium sulfate, the solvent was evaporated under reduced pressure, and the residue was washed with petroleum ether. After drying, 20.3 g of a yellow oil was obtained, with a yield of 91 %, MS (ESI) m / z 223.3 ([M+H] + ).

[0096] (2) Dissolve 0.2 mol of phosphorus pentoxide in 200 ml of methanesulfonic acid, add 0.1 mol of the yellow oil prepared in the first step into it in batches, react at 140 ° C, and after the rea...

Embodiment 2

[0103] Example 2, 7-(4-(4-(2-methoxyphenyl)piperazin-1-yl)butoxy)-2-methyl-3,4-dihydroisoquinoline-1( 2H)-ketone (2)

[0104] Using 1-(2-methoxyphenyl)piperazine instead of 6-fluoro-3-(piperidinyl-4-yl)benzo[d]isoxazole as raw material, the target compound was prepared according to the method of Example 1 , and the structural formula is shown in number (2) in Table 1. 1 H-NMR (600MHz, CDCl 3 )δ1.72-1.86(m,4H),2.50(t,2H,J=12Hz),2.69-2.70(m,3H),2.94(t,2H,J=12Hz),3.12-3.16(m,2H ),3.18(s,3H),3.54(t,2H,J=12Hz),3.87(s,3H),4.05(t,2H,J=6Hz),6.86-6.88(m,1H),6.91-7.07 (m, 5H), 7.61 (d, 1H, J=6Hz). MS (ESI) m / z 424.3 ([M+H] + ).

Embodiment 3

[0105] Example 3, 2-methyl-7-(4-(4-(3-(trifluoromethyl)phenyl)piperazin-1-yl)butoxy)-3,4-dihydroisoquinoline -1(2H)-one(3)

[0106] Use 1-(3-(trifluoromethyl)phenyl) instead of 6-fluoro-3-(piperidinyl-4-yl)benzo[d]isoxazole as raw material, and prepare the target according to the method of Example 1 Compound, structural formula as shown in number (3) in Table 1. 1 H-NMR (600MHz, CDCl 3 )δ1.73-1.88(m, 4H), 2.21-2.22(m, 2H), 2.50(t, 2H, J=12Hz), 2.64-2.66(m, 3H), 2.94(t, 2H, J=12Hz ),3.18(s,3H),3.26-3.28(m,3H),3.55(t,2H,J=12Hz),4.06(t,2H,J=6Hz),6.96-6.98(m,1H),7.06 -7.10(m,3H),7.12-7.14(m,1H),7.34-7.36(m,1H),7.61(d,1H,J=6Hz). MS(ESI) m / z 462.2([M+H ] + ).

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Abstract

The invention relates to the field of medicines, in particular to a lactam derivative and application thereof, and more specifically relates to a lactam derivative and a pharmaceutical composition containing the same as well as application of the composition and the lactam derivative to the preparation of a drug for prevention or treatment of nervous and mental diseases. The lactam derivative has a structure shown as a formula I.

Description

technical field [0001] The present invention relates to the field of medicine, specifically, the present invention relates to a lactam derivative and its application, more specifically, the present invention relates to a lactam derivative, a pharmaceutical composition containing the lactam derivative and the combination and the use of the lactam derivatives in the preparation of prevention or treatment of schizophrenia. Background technique [0002] Schizophrenia has a history of more than one hundred years as an independent disease unit. In 1896, on the basis of summarizing the work of predecessors, Kraepelin summarized several clinical phenomena previously proposed into one disease, which he called dementia praecox; Disorders of volition and autism have at their core schizophrenia, which is still used today. [0003] Schizophrenia is the most serious and harmful disease among all mental diseases, with a global incidence of about 1-2%. The lifetime prevalence of schizoph...

Claims

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Application Information

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IPC IPC(8): C07D413/14C07D217/24C07D405/12C07D417/12C07D401/12C07D239/88C07D239/90A61K31/517A61K31/4725A61K31/506A61K31/496A61K31/536A61P25/18
CPCC07D217/24C07D239/88C07D239/90C07D401/12C07D405/12C07D413/14C07D417/12A61K31/4725A61K31/496A61K31/506A61K31/517C07D221/04C07D409/12A61P25/00A61P25/18A61P25/24
Inventor 陈寅窦飞邱印利于民权张桂森
Owner NHWA PHARMA CORPORATION
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