cas 66104-23-2, Pergolide mesylate salt | Articles data

The development of a high-yield and low environmental impact synthesis able to deliver highly pure pergolide mesylate 1 is described. The process [seven chemical steps (four telescoped), three steps of isolation of intermediate, and only one drying] affords pergolide mesylate 1 in 75-81% overall yield from dihydrolysergic acid 4 with >99.8% purity.

The present invention provides a process for decyanating a pergolide intermediate with an alkali metal hydroxide in an alcoholic solvent having a boiling point greater than about 100° C. at a temperature in the range of about 100° C. to about 175° C.

6-n-Propyl (ethyl or allyl)-8β-methoxy-(methylsulfinyl, methylsulfonyl, or methylmercapto) methylergolines, 8-ergolenes or 9-ergolenes, useful as prolactin inhibitors and in the treatment of Parkinsonism.

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66104-23-2

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Chemical Properties

Appearance/Colour :White to off-white solid

Melting Point: 252-254 °C

Boiling Point: 491.3 °C at 760 mmHg

Flash Point:250.9 °C

Solubility:ethanol: soluble2mg/mL

Storage Temp.:−20°C

PKA: pKa (66% DMF) 7.8(at 25℃)

PSA: 107.08000

LogP: 4.79380

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