o-Chloro-α-(tert-butylaminomethyl)benzylalcohol Hydrochloride(C-78)および関連化合物の合成と気管支拡張作用

越中 栄一; 倉田 栄; 山岸 輝里; 久保 信治; 加藤 日出男

doi:10.1248/yakushi1947.98.9_1198

Synthesis and Bronchodilating Activity of o-Chloro-α-(tert-butylaminomethyl)-benzylalcohol Hydrochloride (C-78) and Related Compounds

EIICHI KOSHINAKA, SAKAE KURATA, KAGARI YAMAGISHI, SHINJI KUBO, HIDEO KATO

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Keywords: o-chlorobenzylalcohol derivative, phenylglyoxal derivatives, bronchodilator, β₂-stimulant, 2-chloro-4-hydroxybenzylalcohol derivative

JOURNAL FREE ACCESS

1978 Volume 98 Issue 9 Pages 1198-1207

DOI https://doi.org/10.1248/yakushi1947.98.9_1198

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Abstract

For the development of a new bronchodilator, chloro-substituted α-(tert-butylamino-methyl) benzyl alcohols (VIIa-c) were synthesized via glyoxal derivatives. Further, hydroxy-substituted derivatives (VIII, IXa-e) of VIIa were synthesized by several methods. Among these compounds, o-chlorobenzyl alcohol hydrochloride (C-78) had a strong effect, and its 4-hydroxy derivative showed a strong effect, comparable to Salbutamol.

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