Process for the preparation of 1,2,3,4,8,9,10,10a-octahydro-7bH-cyclopenta [b] [1,4] diazepino- [6,7,1-hi] indole derivatives

A process for preparing compounds of the formula:

• 32
• wherein:
• R1, R2, R4 and R5 are each independently, hydrogen, hydroxy, alkyl of 1-6 carbon atoms, cycloalkyl, alkoxy of 1-6 carbon atoms, halogen, fluorinated alkyl of from 1 to 6 carbon atoms, —CN, —NH—SO2-alkyl of 1-6 carbon atoms, —SO2—NH-alkyl of 1-6 carbon atoms, alkyl amide of 1-6 carbon atoms, amino, alkylamino of 1-6 carbon atoms, dialkylmino of 1-6 carbon atoms per alkyl moiety, fluorinated alkoxy of 1-6 carbon atoms, acyl of 2-7 carbon atoms, aryl or aroyl;
• R3 is hydrogen, alkyl of 1-6 carbon atoms, cycloalkyl, alkoxy of 1-6 carbon atoms, fluorinated alkyl of from 1 to 6 carbon atoms, alkyl sulfonamide of 1-6 carbon atoms, alkyl amide of 1-6 carbon atoms, amino, alkylamino of 1-6 carbon atoms, dialkylmino of 1-6 carbon atoms per alkyl moiety, fluorinated alkoxy of 1-6 carbon atoms, acyl of 2-7 carbon atoms, aryl or aroyl;
• the process comprising the steps of:
• a) acylating a cyclopentaindole methylamine of the formula:
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• wherein R1, R2, R4 and R5 are with an acylating agent of the formula:
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• wherein R3 is as defined above and L represents a leaving group to produce a acylated compound of the formula:
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• b) cyclizing the acylated compound of step a) to produce an optionally substituted Diazabenzo[cd]cyclopenta[a]azulen-6-one compound of the formula:
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• and
• c) reducing the Diazabenzo[cd]cyclopenta[a]azulen-6-one compound of step b) to produce an optionally substituted Diazabenzo[cd]cyclopenta[a]azulene compound of the formula:
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