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Scheme 1 | BMC Chemistry

Scheme 1

From: Discovery of novel 2,3,4,5-tetrahydrospiro[benzo[c]azepine-1,1’-cyclohexan]-5-ol derivatives as PARP-1 inhibitors

Scheme 1

Reactions and conditions: (i) Mg, cyclohexanone, ethoxyethane, 35℃, 3 h; (ii) NaN3, 20℃, 12 h; (iii) LiAlH4, 40℃, 12 h; (iv) Methyl-acrylate, no solvent required, 40℃, 12 h; (v) NaOH, water, 50℃, 2 h; (vi) SOCl2, 35℃, 2 h; (vii) AlCl3, 25℃, 24 h; (viii) 3-bromoprop-1-yne, 70℃, 12 h; (ix) LiAlH4, 60℃, 12 h; (x) Corresponding azidebenzene, 35℃, 9 min, 71.91-84.00%

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