"Hokunarin Tape" used to treat asthma and bronchitis

Tulobuterol (INN) is a long-acting beta2-adrenergic receptor agonist, marketed in Japan as a transdermal patch under the name Hokunalin tape (ホクナリンテープ).[1]

Currently, it is only legal in 7 countries: Japan, Germany, China, South Korea, Bangladesh, Pakistan, and Venezuela. It is available in India also.

Synthesis

The oxidation of 2'-chloroacetophenone (1) with selenium dioxide gives o-chlorophenylglyoxal (2). Condensation with tert-butylamine gives the imine (3). Reduction with sodium borohydride completes the synthesis of tulobuterol.[2]

References

  1. ^ Horiguchi T, Kondo R, Miyazaki J, Fukumokto K, Torigoe H (2011). "Clinical evaluation of a transdermal therapeutic system of the beta2-agonist tulobuterol in patients with mild or moderate persistent bronchial asthma". Arzneimittel-Forschung. 54 (5): 280–5. doi:10.1055/s-0031-1296971. PMID 15212190. S2CID 9765046.
  2. ^ Wu CJ, Peng P, Xia LT, Liu X, Yu CX, Zheng ZB, et al. (2023). "Development of a New Process for Tulobuterol Hydrochloride". Pharmaceutical Fronts. 05: e31 – e37. doi:10.1055/s-0043-1764464.
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