43229-01-2

1-(4-(Benzyloxy)-3-nitrophenyl)-2-bromoethanone, can be used as an intermediate in the synthesis of Arformoterol Tartrate (A767505), which is a derivative of Arformoterol, a long acting beta-adrenoceptor agonist drug indicated for the treatment of chronic obstructive pulmonary disease (COPD).

Step 2: 200 g of 4-benzyloxy-3-nitroacetophenone (Intermediate 1) was dissolved in 1000 mL of dichloromethane and 277 g of trimethylphenylammonium tribromide was added. The reaction mixture was heated to 300 °C and kept for 4 hours. After completion of the reaction, the residual liquid was poured into water, filtered, washed and dried to give 253 g of 3'-nitro-4'-benzyloxy-2-bromoacetophenone in 98% yield.

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