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Novel medicinal salt for cinepazide and preparation method thereof

A medicinal salt and pharmacy technology, applied in the field of medicine, can solve problems such as hidden dangers of clinical drug safety, inconvenient drug production, storage, transportation and use, and light sensitivity

Inactive Publication Date: 2007-10-24
车冯升
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] However, the raw material of cinepazide maleate and its injection are extremely sensitive to light, and have poor photostability. They need to be protected from light and kept in airtight storage during storage, which brings great inconvenience to the production, storage, transportation and use of the drug. At the same time, it also brings hidden dangers to the guarantee of clinical safety drug use.

Method used

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  • Novel medicinal salt for cinepazide and preparation method thereof
  • Novel medicinal salt for cinepazide and preparation method thereof
  • Novel medicinal salt for cinepazide and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0101] The preparation of embodiment 1 cinepazide mesylate

[0102] Take cinepazide 10g (24mmol), put it into the reaction bottle, add 50ml ethanol, stir to dissolve, then add dropwise 2.9g methanesulfonic acid (25mmol) / 50ml ethanol under stirring, let stand for 1h after the dropwise addition, the reaction solution Freeze and crystallize to obtain the off-white cinepazide mesylate crude product; add the crude product to 90ml of ethanol, stir and heat to reflux, and after the solid is completely dissolved, the solution is cooled and crystallized to obtain 9.5 g of white crystalline powder, yield: 77.2%.

[0103] 1 H-NMR (600MHz, DMSO) δ: 1.94[m, 4H], 2.33[s, 4H], 3.21[brs, 4H], 3.39[t, 4H], 3.56[brs, 2H], 3.69[s, 9H] ], 4.26[s, 2H], 4.50[brs, 2H], 7.08[s, 2H], 7.22[d, 1H], 7.52[d, 1H], 10.17[brs, 1H]

[0104] IR(KBr)cm -1 : 3442, 2951, 2868, 2585, 1657, 1448, 1425, 1271, 1232, 1035, 765, 557, 531

[0105] Elemental analysis (C 22 h 31 N 3 o 5 ·CH 3 SO 3 h)

[0106] ...

Embodiment 2

[0108] The preparation of embodiment 2 cinepazide nitrate

[0109] Take cinepazide 15g (36mmol), put it into the reaction bottle, then add 60ml of 95% ethanol, stir to dissolve, then add 2.4g of nitric acid (about 36mmol) / 10ml of ethanol dropwise under stirring, let stand for 1h after the dropwise addition, and react Liquid freezing and crystallization, the off-white cinepazide hydrochloride crude product was obtained; the crude product was added to 80ml ethanol / 15ml water, stirred and heated to reflux, after the solid was completely dissolved, the solution was cooled and crystallized to obtain 14.8g of white crystalline powder, the yield : 85.4%.

[0110] 1 H-NMR (600MHz, DMSO) δ: 2.01[m, 4H], 3.29[brs, 4H], 3.31[t, 4H], 3.61[brs, 2H], 3.67[s, 9H], 4.18[s, 2H] ], 4.55 [brs, 2H], 7.04 [s, 2H], 7.35 [d, 1H], 7.47 [d, 1H], 10.21 [brs, 1H]

[0111] IR(KBr)cm -1 : 3427, 2942, 2940, 2845, 1633, 1597, 1530, 1436, 1222, 1069, 847, 565, 528

[0112] Elemental analysis (C 22 h 3...

Embodiment 3

[0115] The preparation of embodiment 3 cinepazide phosphate

[0116] Take cinepazide 15g (36mmol), put it into the reaction bottle, then add 80ml of ethanol, stir to dissolve, then add dropwise 4.2g of phosphoric acid (36mmol) / 10ml of ethanol under stirring, stir for 1h after the dropwise addition, and let stand for 1h, The reaction solution was frozen and crystallized to obtain the crude product of off-white cinepazide phosphate; the crude product was added to 70ml of ethanol / 10ml of water, stirred and heated to reflux, and the solution was cooled and crystallized after the solid was completely dissolved to obtain 15.7g of white crystalline powder. Rate: 84.8%.

[0117] 1 H-NMR (600MHz, DMSO) δ: 2.04[m, 4H], 3.11[brs, 4H], 3.26[t, 4H], 3.49[brs, 2H], 3.78[s, 9H], 4.22[s, 2H] ], 4.60 [brs, 2H], 7.05 [s, 2H], 7.42 [d, 1H], 7.55 [d, 1H], 10.21 [brs, 3H]

[0118] IR(KBr)cm -1 : 3436, 2947, 2938, 2845, 1631, 1609, 1515, 1436, 1227, 1068, 847, 562, 527

[0119] Elemental analy...

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Abstract

The invention discloses a new medicinal salt of (E)-1-{4-[(3',4',5'-trimethoxy cinnamon acyl]-1-piperazidine} acetopyrrole as cinprazole, which comprises the following parts: mesilate, phosphate, nitrate, sulfate, hydrobromide, p-toluenesulfonic acid salt, tartrate, fumarate, citrate, succinate, malonate, optimizing the mesilate, nitrate, phosphate and sulfate, for mesilate at best. The drug can be used to treat and / or prevent cardiovascular and cerebrovascular disease and peripheral vessel disease. The drug possesses good stability and superior solubility, which can be made into acceptable pharmacy agent.

Description

1. Technical field [0001] The present invention relates to (E)-1-{4-[(3',4',5'-trimethoxycinnamoyl)]-1-piperazine}acetylpyrrolidine, a new pharmaceutically acceptable salt of cinepazide The preparation method and application thereof belong to the technical field of medicine. 2. Background technology [0002] Cardiovascular and cerebrovascular diseases are currently the number one cause of death, and are common and frequently-occurring diseases that seriously threaten the health of our people. Choosing effective and safe therapeutic drugs is an important issue for clinicians. Cinepazide is widely used all over the world because of its definite curative effect and small adverse reactions. The chemical name of cinepazide is: (E)-1-{4-[(3′,4′,5′-trimethoxycinnamoyl)]-1-piperazine}acetylpyrrolidine, the structural formula is as follows: [0003] [0004] Cinepazide Maleate (Cinepazide Maleate) is the maleate of cinepazide, developed by the French Sanofi-Aventis company, firs...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D295/18A61K31/496A61P9/00
Inventor 车冯升
Owner 车冯升
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