Process and intermediates for the preparation of olanzapine
AssigneeKRKA, Tovarna Zdravil, D.D.
InventorsRoman Lenarsic, Rok Zupet, Milena Benedik, Barbara Mohar, Anton Stimac
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Abstract
The invention provides an improved process for preparing Olanzapine as well as intermediates therefor.
Claims11
Process for the manufacture of Olanzapine of the following formula I or a salt thereof:
- by converting a compound of the following formula II or a salt thereof
- in which
- (i) R1 and R2 together form ═CH—CH2—CH3, or
- (ii) R1 and R2 are both H, or
- (iii) R1 is H and R2 is —CH(R3) —CH2—CH3, wherein R3 is a leaving group that can be eliminated together with R1 to result in R1 and R2 together forming ═CH—CH2—CH3, to give Olanzapine or a salt thereof.
The compound according to claim 11, which is benzodiazepine of the following formula IV:
- or salts thereof.
The compound according to claim 11, which is benzodiazepine-propanol of the following formula VI:
- or salts thereof.
The compound according to claim 11, which is benzodiazepine-ester of the following formula VII:
- in which R4 is selected from the group of acyl and sulfonyl and preferably is trifluoroacetyl or methane sulfonyl, or salts thereof.
Use of a compound according to claim 11 for the manufacture of Olanzapine.
A compound of the following formula
- in which
- (i) R1 and R2 together form ═CH—CH2—CH3, or
- (ii) R1 and R2 are both H, or
- (iii) R1 is H and R2 is —CH(OR3) —CH2—CH3, wherein R3 is selected from the group of hydrogen, acyl and sulfonyl and preferably is trifluoroacetyl or methane sulfonyl, or salts thereof.
Dependencies are inferred from the claim text.