Arrowsmith, John E. published the artcileLong-acting dihydropyridine calcium antagonists. 1. 2-Alkoxymethyl derivatives incorporating basic substituents, Safety of 2-(Benzyl(methyl)amino)ethanol, the publication is Journal of Medicinal Chemistry (1986), 29(9), 1696-702, database is CAplus and MEDLINE.
Aminoalkoxymethyldihydropyridines I [R = Ph, substituted Ph, 1-naphthyl, 2-thienyl, 4-pyridyl; R1 = (un)substituted NH2; n = 2, 3] were prepared from RCHO, R1(CH2)nOCH2COCH2CO2Et, and H2NCMe:CHCO2Me or via I (R = N3, phthalimido). Their potencies as Ca antagonists were determined I (R = 2-ClC6H4, R1 = NH2, n = 2) (amlodipine) was comparable in potency to nifedipine and had an elimination half-life of 30 h in dogs. Oral bioavailability approached 100%, and hemodynamic responses were gradual in onset and long-lasting in effect. The two enantiomers were prepared; the bulk of the activity resided with the (-)-isomer. X-ray crystallog. studies, carried out on I (R = 2-ClC6H4, R = morpholinosulfonyl, n = 2) suggest the existence of a weak H bond between the side-chain O and the H on the ring N.
Journal of Medicinal Chemistry published new progress about 101-98-4. 101-98-4 belongs to alcohols-buliding-blocks, auxiliary class Amine,Benzene,Alcohol, name is 2-(Benzyl(methyl)amino)ethanol, and the molecular formula is C10H15NO, Safety of 2-(Benzyl(methyl)amino)ethanol.
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