Method of making diazepine derivatives
AssigneeHoffmann-La Roche Inc.
InventorFabienne Hoffmann-Emery
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Abstract
The present invention relates to a process for manufacturing diazepine derivatives of the general formula I wherein R1 is lower alkyl and R2 is hydrogen, or R1 and R2 are together —(CH2)n— and n is 2 or 3; R3 is halogen, lower alkyl, lower alkoxy and m is 0, 1 or 2; R4 is hydrogen or lower alkyl. The compounds of general formula I are valuable intermediate products for the manufacture of imidazo [1,5-a][1,4]diazepine derivatives, like for instance 7-chloro-3-(5-dimethylaminomethyl-[1,2,4]oxadiazol-3-yl)-5-methyl-4,5-dihydro-imidazo[1,5-a][1,4]benzodiazepin-6-one, which diazepine derivatives show excellent psychopharmacological properties as agonists of the central benzodiazepine receptors.
Claims20
A process for manufacturing a compound of formula I
- wherein:
- R1 is lower alkyl;
- R2 is hydrogen;, or
- R1 and R2 are together —(CH2)n— and n is 2 or 3;
- R3 is halogen, lower alkyl, lower alkoxy and m is 0, 1 or 2;
- and
- R4 is hydrogen or lower alkyl:
- comprising, reacting a compound of formula II
- with a compound of formula III
- wherein R1, R2, R3, R4, m and n have the meanings set forth above, and said reaction between said compound of formula II and said compound of formula III takes place in the presence of an apolar solvent.
Dependencies are inferred from the claim text.