Hydrochloric Acid → 3-Bromo-4-fluorobenzenesulfonamide

HRID 575602Notes

Reaction equation

HRID 575602 reaction equation
[Br:1][C:2]1[CH:3]=[C:4]([S:9](Cl)(=[O:11])=[O:10])[CH:5]=[CH:6][C:7]=1[F:8].C(Cl)Cl.[OH-].[NH4+:17].Cl>C1COCC1>[Br:1][C:2]1[CH:3]=[C:4]([S:9]([NH2:17])(=[O:11])=[O:10])[CH:5]=[CH:6][C:7]=1[F:8]

Participants

6

Conditions

Temperature
0 °C

Procedure

A solution of 3-bromo-4-fluorobenzenesulfonyl chloride (1 g, 3.3 mmol, 90% pure) stirred at 0° C. in THF (15 ml) and DCM (5 ml) was treated with aqueous ammonium hydroxide (28%) by dropwise addition over 15 min. After stirring at 0° C. for 210 min, the mixture was acidified (pH=1) by addition of 1 N HCl (aq). After the mixture was concentrated in vacuo to near dryness, it was treated with water (50 ml), sonicated for 3 min and filtered. After the filter cake was washed sequentially with water (50 ml) and hexanes (100 ml), it was dried in vacuo to afford the title compound (503 mg, 60%) as a white solid which was carried forward without purification. LCMS (M−H)−=253.

Workup

  1. concentrationAfter the mixture was concentrated in vacuo
  2. additionwas treated with water (50 ml)
  3. customsonicated for 3 min
  4. filtrationfiltered
  5. washAfter the filter cake was washed sequentially with water (50 ml) and hexanes (100 ml), it
  6. customwas dried in vacuo

Sources & evidence

ORD record
ord-e0b1cadaf92749d8a05bbfaf10a4b409
Source dataset
uspto-grants-2015_05
Patent number
US09034900B2

Reaction notes

Loading…