1,8-Diazabicyclo(5.4.0)undec-7-ene → Benzo[b]thiophene, 6-bromo-5-fluoro-

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Reaction Steps

Using analogous reaction condition and reagents as described in Example 25 for the preparation of I-25c above, 6-bromo-5-fluoro-benzo[b]thiophene-2-carboxylic acid (I-27c: 250 mg 0.89 mmol) in DMA (4 mL) and DBU (550 mL, 3.6 mmol) were heated in microwave to afford the crude product. Purification by column chromatography on silica gel (100% hexane) afforded 180 mg of the product (86% yield).

Provenance & Evidence