Patent ID: 7141563

Claim:
A process for synthesis of a compound of the formula: wherein R 1 , R 2 , R 4 and R 5 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—SO 2 -alkyl of 1–6 carbon atoms, —SO 2 —NH-alkyl of 1–6 carbon atoms, alkyl amide of 1–6 carbon atoms, amino, alkylamino of 1–6 carbon atoms, dialkylamino of 1–6 carbon atoms per alkyl moiety, fluorinated alkoxy of 1–6 carbon atoms, acyl of 2–7 carbon atoms, aryl or aroyl; R 3 is hydrogen, alkyl of 1–6 carbon atoms, cycloalkyl, alkoxy of 1–6 carbon atoms, fluorinated alkyl of from 1 to 6 carbon atoms, —NH—SO 2 -alkyl of 1–6 carbon atoms, —SO 2 —NH-alkyl of 1–6 carbon atoms, alkyl amide of 1–6 carbon atoms, amino, alkylamino of 1–6 carbon atoms, dialkylamino 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) treating a cyclopenta[b]indoline compound of the formula: with an electrophile to form an optionally substituted acetamide compound of the formula: b) treating the optionally substituted acetamide of step a) with a reducing agent to form the corresponding optionally substituted cyclopenta[b]indol-4-yl-amine of the formula: c) treating the cyclopenta[b]indol-4-yl-amine of step b) with an aldehyde in the presence of an acid to form an optionally substituted diaza-benzo[cd]cyclopenta[a]azulene compound of the formula: