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filingDate 1973-02-02-04:00^^<http://www.w3.org/2001/XMLSchema#date>
grantDate 1975-09-23-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_8e57a8f3f81e66a39679f15ccf101f1d
http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_53cba9d47bd2e1691b602952d49ad7ea
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publicationDate 1975-09-23-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber US-3907812-A
titleOfInvention Butyrophenone derivatives
abstract A novel process for preparing central nervous system active butyrophenone derivatives in which gamma piperidinobutyrophenone derivatives of the formula, wherein R1 is hydrogen, halogen, amino, acylamino, alkylamino or N-acylalkylamino; R2 is hydrogen or halogen; R3 is hydrogen or unsubstituted or alkyl-, alkoxy-, halogen- or trifluoromethylsubstituted phenyl; and R4 is hydrogen or hydroxyl, can be prepared by reacting an indole derivative of the formula, wherein R2, R3 and R4 are as defined above, and R5 and R6 are each independently hydrogen or alkyl, with an oxidizing agent to yield an o-acylamino- gamma -piperidinobutyrophenone derivative of the formula, wherein R2, R3, R4, R5 and R6 are as defined above, and further, if necessary, hydrolyzing the product to yield an o-amino- gamma -piperidinobutyrophenone derivative of the formula, wherein R2, R3, R4 and R5 are as defined above, and further diazotizing, if desired, in case R5 is hydrogen, the obtained oamino- gamma -piperidinobutyrophenone derivative and subsequently decomposing the resultant diazonium compound to replace the diazonium group by hydrogen or halogen. Among the butyrophenone derivatives thus obtained, those in which R1 is halogen, amino, acylamino, alkylamino or N-acylalkylamino are novel compounds.
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