ceftaroline intermediate synthesis

4synthesis methods

Product Name:ceftaroline intermediate
CAS Number:1427207-46-2
Molecular formula:C9H8N2S2
Molecular Weight:208.3

Pyridinium, 4-[2-(acetylthio)-4-thiazolyl]-1-methyl-, iodide (1:1)

1427207-45-1
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1427207-46-2
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Yield:1427207-46-2 15.0g

Reaction Conditions:

with sodium hydrogencarbonate in methanol at 0; pH=7.6 - 8.0; for 4 h;

Steps:

4 Example 4: r4-(N-MethvIpyridinium-4-vl)-1 ,3-thiazof-2-yi|thiolate

34.5g N-Methyl-4-(2-acetylthio-1 ,3-thiazol-4-yl)pyridinium iodide were dissolved in 360ml MeOH/240mi water and cooled to 0°C. The pH was adjusted to 7.6 to 8.0 by addition of saturated sodium bicarbonate solution and the mixture was stirred for 4h. The crystals were filtered and washed with 60ml water and dried in vacuo. Yield: 15.0g H-NMR (DMSO-c/e) δ 4.22{s, 3H), 8.06(s, 1 H), 8.30(d,2H; J=6,7Hz), 8,78(d,2H; J=6,7Hz) ¹ C-NMR (DMSO-d₆) δ 46.7, 122.0, 122.2, 144.9, 147.2, 147.8, 186.3

References:

WO2013/34718,2013,A1 Location in patent:Page/Page column 17

77168-63-9 Synthesis

77168-63-9
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1427207-46-2
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References

1122-54-9
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1427207-46-2
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References

Ethanethioic acid, S-[4-(4-pyridinyl)-2-thiazolyl] ester

1427207-44-0
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1427207-46-2
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References