- Preparation method of nitrogen unsubstituted pyrazole and indazole boric acid
-
The invention discloses a method for preparing nitrogen unsubstituted pyrazole and indazole boric acid. Nitrogen unsubstituted halogenated pyrazole and a derivative thereof, or nitrogen unsubstitutedhalogenated indazole and a derivative of the nitrogen unsubstituted halogenated indazole react with triisopropylchlorosilane in an organic solvent to generate a triisopropylsilyl protected halogenatedpyrazole or halogenated indazole compound, then a lithium-bromine exchange reaction is carried out with n-butyl lithium, a borate is added to introduce boron atoms, and the nitrogen unsubstituted pyrazole or indazole boric acid is obtained in high yield after hydrolysis.
- -
-
Paragraph 0061-0063; 0067-0070
(2020/01/12)
-
- Substituted 5-benzyl-2,4-diaminopyrimidines
-
The invention relates to substituted 5-benzyl-2,4-diaminopyrimidines of general formula (A) wherein R1is C2-C3 alkyl an R2is heterocyclyl, phenyl or naphthyl, bonded by one of its C-atoms and R3is C2-C6 alkyl, alkenyl, cycloalkyl, cycloalkylalkyl, heterocyclylalkyl, alkylsulfonyl, cycloalkylsulfonyl, cycloalkylalkylsulfamoyl, heterocyclysylfonyl, heterocyclylalkylsulfonyl or dialkylsulfamoyl; wherein alkyl, cycloalkyl and alyenyl can carry up to 6 carbon atoms alone or in compositions and can carry up to 6 ring members heterocyclically, alone, or in compositions and the groups R2and R3can be substituted; and to acid addition salts of compounds. The invention also relates to a method for producing the above 5-benzyl-2,4-diaminopyrimidines, to the intermediate. products that are produced, to corresponding medicaments and to the use of 5-benzyl-2,4-diaminopyrimidines as medicinal preparations. The products have antibiotic properties and are useful for combating or preventing infectious diseases.
- -
-
Page column 24
(2010/02/09)
-