DE2530577

Procedure for preparing ergoline derivatives, of formula I, ** (See formula) ** where X is hydrogen, chlorine or bromine, R1 is methyl or ethyl, and R2 is CH2-CN, or a group NR3R4, where R3 is hydrogen or alkyl of 1 to 4 carbon atoms, and is formyl, alkanoyl of 2 to 5 carbon atoms in its entirety, a...

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Hauptverfasser: FEHR, THEODOR, DORNACH, CH, STUETZ, PETER, REINACH, CH, STADLER, PAUL, BIEL-BENKEN, CH
Format: Patent
Sprache:eng
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Zusammenfassung:Procedure for preparing ergoline derivatives, of formula I, ** (See formula) ** where X is hydrogen, chlorine or bromine, R1 is methyl or ethyl, and R2 is CH2-CN, or a group NR3R4, where R3 is hydrogen or alkyl of 1 to 4 carbon atoms, and is formyl, alkanoyl of 2 to 5 carbon atoms in its entirety, alkoxycarbonyl of 2 to 5 atoms carbon in all of it, mono- to trihalogenalkoxycarbonyl of 3 to 5 carbon atoms in all of it, the alkoxy radical thereof being replaced by halogen in a position other than the α relative to oxygen, or the radical SO2R5, where R5 is alkyl of 1 to 4 carbon atoms, mono- to trihalogenalkyl of 1 to 4 carbon atoms, phenyl, pyridyl, phenyl monosubstituted by halogen or alkoxy of 1 to 4 carbon atoms, or a group NR6R7, where each of R6 and R7, independently, is hydrogen or C 1-4 -alkyl, or R6 and R7 together are one of the groups (CH2) not (Ch2) 2-A- (CH2) 2, where n is a number from 3 to 7, and A is oxygen, sulfur, or nitrogen substituted by alkyl of 1 to 4 carbon atoms or phenyl, characterized in that a) a compound of formula Ia is produced, ** ( See formula) ** where X and R1 have the previously indicated meanings, exchanging the radical Z for a cyano group in a compound of formula II, ** (See formula) ** where Z is a radical capable of being interchanged in a nucleophilic substitution reaction, and X and R1 have the previously indicated meanings, or b) a compound of formula Ib is produced, ** (See formula) ** where X, R1, R3 and R4 have the previously indicated meanings, acylating a compound of formula III, where X, R1 and R3 have the previously indicated meanings, with a reactive functional derivative of an acid R4OH, where R4 has the previously indicated meaning. (Machine-translation by Google Translate, not legally binding)