22525-99-1Relevant articles and documents
Design, synthesis and evaluation of racemic 1-(4-hydroxyphenyl)-2-[3- (substituted phenoxy)-2-hydroxy-1-propyl]amino-1-propanol hydrochlorides as novel uterine relaxants
Viswanathan,Kodgule,Chaudhari
, p. 3532 - 3535 (2005)
Novel 1-(4-hydroxyphenyl)-2-[3-(substituted phenoxy)-2-hydroxy-1-propyl] amino-1-propanol hydrochlorides were designed based on the pharmacophore for potent uterine relaxant activity and by utilizing the principles of structural hybridization. The designed molecules were synthesized as racemates by a novel route and were evaluated for uterine relaxant activity in vitro on isolated rat uterus and in vivo in pregnant rats. Their cAMP-releasing potential was studied using rat uterus tissue homogenates by the cAMP [3H] assay, and cardiac stimulant potential was evaluated on isolated guinea pig right atrium. All compounds exhibited potent uterine relaxant activity in vitro and produced a significant delay in the onset of labour in pregnant rats; their cAMP-releasing potential was slightly less, while their cardiac stimulant potential was insignificant as compared to isoxsuprine hydrochloride.
Method for diacetate intermediate 5 - acetamide group -2 - (2, 3 - epoxypropoxy) acetophenone
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Paragraph 0023; 0026; 0028-0029; 0031-0032; 0034-0035..., (2021/11/14)
The invention belongs to the field of organic photochemical and drug intermediate chemistry. The invention particularly relates to a method for synthesizing diacetate intermediate - acetamide group 5 - (-2 - 2 epoxypropoxy) acetophenone containing acetylated 3 - photochemical rearrangement reaction in series. The reactant is cooled to the polar organic solvent, Fries rearrangement is carried out directly by ultraviolet - visible light irradiation with specific wavelength, and the intermediate Fries acetyl 2 -4 - acetyl aminophenol is obtained by heating and evaporating the solvent after the reaction is finished. Sodium hydroxide was added to prepare the phenol salt. Then, an intermediate 5 - acetamide group -2 - (2, 3 - epoxypropoxy) acetophenone was obtained by reaction with epichlorohydrin. The tandem type synthesis method disclosed by the invention is simple and feasible, and low-toxicity, high-efficiency and cheap green chemical reagents are used in the synthesis process.