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0 °C

Dimethyl 13-cyclohexyl-6,7-dihydro-5H-indolo[2,1-a][2]benzazepine-6,10-dicarboxylate (prepared according to International patent application publication WO 2006/020082) was dissolved in anhydrous THF (0.02 M) and after cooling at 0° C. BH3THF complex (1.5 eq.) was added followed by LiBH4 (1 eq.) and water (4 eq.). The mixture was left stirring at RT for 2h, then 1N hydrochloric acid was slowly added. The crude was extracted twice with EtOAc, dried over Na2SO4, filtered, and all volatiles were removed in vacuo to obtain desired compound as a yellow solid (85%) that was used in the next step without purification. (ES+) m/z 404 (M+H)+.

1. additionBH3THF complex (1.5 eq.) was added
2. waitThe mixture was left
3. extractionThe crude was extracted twice with EtOAc
4. dry with materialdried over Na2SO4
5. filtrationfiltered
6. customall volatiles were removed in vacuo