Abstract
New β-adrenergic stimulants, 3-acylamino-4-hydroxy-α-(N-substituted aminomethyl)-benzyl alcohols (VIII) were prepared via 3-amino-4-benzyloxy-α-(N-substituted aminomethyl) benzyl alcohols (V) in several steps. These agents were catecholamine derivatives, in which m-phenolic OH was replaced by acylamino and substituted acylamino groups. Terbutaline analogues (XIXa, b, XX), in which one or both of two phenolic OH were replaced by formamido or methoxycarboxamido groups were synthesized, too. Compounds (VIIIa, c, 1-q) bearing formylamino group in the meta position showed potent β2-stimulant activity in vitro. In these, N-phenylalkyl series were more potent β2-stimulant than N-alkyl series. Several compounds, which bear two asymmetric centers, were separated into two racemates and the β2-stimulant activity of them were different. From these compounds, 3-formamido-4-hydroxy-α-(N-(p-methoxy-α-methylphenethyl) aminomethyl)-benzyl alcohol ·1/2 fumarate (VIIIn-A) (BD-40-A) was selected as the best compound.
Sign-in/Register to access full text options 
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a callDisclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.
