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US 7,064,216 B2Granted
Condensation reagents and a process for their preparation
AssigneeBayer Aktiengesellschaft
InventorsJoachim Rudolph, Ralf Wischnat
Life of this patent
Estimating the term…
Abstract
The present invention relates to new bromo- and chlorothiazolium salts of the formula (I) in which R1, R2, R3, R4, n and X− have the meaning indicated in the disclosure, a process for their preparation, their use as condensation reagents, particularly as peptide coupling reagents, and intermediates for the preparation of these compounds.
Claims5
A compound of the formula (I)
- in which
- R1 represents methyl, ethyl, n-propyl, isopropyl, hydroxyl, methylsulfonyl, ethylsulfonyl, phenylsulfonyl, p-methylphenylsulfonyl, or benzyl that is optionally substituted by halogen, nitro, C1-C4-alkyl, trifluoromethyl, or C1-C4-alkoxy,
- R2 and R3 together represent —(CH2)n— that is optionally substituted by halogen, NO2, carboxyl, carbonyl, C1-C4-alkyl, C1-C4-halogenoalkyl, C1-C4-alkoxy, or C1-C4-halogenoalkoxy or the optionally halogen-, NO2—, C1-C4-alkyl-, C1-C4-halogenoalkyl-, C1-C4-alkoxy-, or C1-C4-halogenoalkoxy-substituted groups having the formulas
- where the arrows mark the points of linkage to the thiazole ring, and n represents 3, 4 or 5,
- R4 represents bromine or chlorine, and
- X− represents chloride, bromide, iodide, hydrogen sulfate, ½ equivalent of sulfate, sulfate, hexachloroantimonate, methanesulfonate, trifluoromethanesulfonate, p-toluenesulfonate, tetrafluoroborate, tetraphenylborate, or hexafluorophosphate.
3 more elements
A compound of the formula (I-2)
- in which
- R1 represents methyl, ethyl, n-propyl, isopropyl, hydroxyl, methylsulfonyl, ethylsulfonyl, phenylsulfonyl, p-methylphenylsulfonyl, or benzyl that is optionally substituted by halogen, nitro, C1-C4-alkyl, or C1-C4-alkoxy,
- R2 and R3 together represent —(CH2)n— that is optionally substituted by halogen, NO2, carboxyl, carbonyl, C1-C4-alkyl, C1-C4-halogenoalkyl, C1-C4-alkoxy, or C1-C4-halogenoalkoxy or the optionally halogen-, NO2—, C1-C4-alkyl-, C1-C4-halogenoalkyl-, C1-C4-alkoxy-, or C1-C4-halogenoalkoxy-substituted groups having the formulas
- where the arrows mark the points of linkage to the thiazole ring, and n represents 3, 4 or 5,
- R4 represents bromine or chlorine, and
- X″− represents tetrafluoroborate, tetraphenylborate, or hexafluorophosphate.
3 more elements
Dependencies are inferred from the claim text.