Synthesis and antiestrogenic activity of the compounds related to the metabolites of (E)-4-[1-[4-[2-(dimethylamino)ethoxy]phenyl]- 2-(4-isopropylphenyl)-1-butenyl]phenyl monophosphate (TAT-59) [corrected

The metabolites of (E) [corrected]-4-[1-[4-[2-dimethylamino)ethoxy]phenyl]- 2-(4-isopropylphenyl)-1-butenyl]phenyl monophosphate, TAT-59, (1), a potent antitumor agent for hormone-dependent tumors, and derivatives of TAT-59 were synthesized to confirm its proposed structure. The structure and the Z-configuration of the metabolites (2a-8a) were confirmed by comparison with synthesized authentic compounds. All of the metabolites and the derivatives of TAT-59 were tested for a binding affinity toward estrogenic receptors in vitro and antiuterotrophic activity in vivo. Most of the metabolites possessed remarkable binding affinity toward estrogenic receptors as well as fairly good antiuterotrophic activity.     

Indole Derivatives. 142. Some Properties of [4-(2-Indolyl)phenyl]phenylmethane and 1-[4-(2-Indolyl)phenyl]-2-phenylethane

The reactions of 2-arylindoles with strong electrophiles take place with significant resin formation. It was shown that electrophilic substitution is directed into the indole ring and into the side chain. 1,7-Migration of the substituent is observed in the investigated systems.     

[4-(4-苯甲酰基苯氧基)苯]苯基碘鎓六氟磷酸盐的合成

紫外光固化反应分为自由基固化机理、阳离子固化机理,以及自由基-阳离子混杂固化机理。自由基-阳离子混杂固化是指在同一体系里同时发生自由基光聚合反应和阳离子光聚合反应[1],结合了前两类聚合反应的优点,表现出很好的协同效应[2]。[4-(4-苯甲酰基苯氧基)苯]苯基碘鎓六氟磷酸     

Synthesis of Methyl-N-[4-(3-R-amino-2-hydroxypropoxy)phenyl]carbamates

By alkylation of methyl-N-(4-hydroxyphenyl)carbamate with (chloromethyl)oxirane in acetone in the presence of K₂CO₃ methyl-N-[4-(2,3-epoxypropoxy)phenyl]carbamate was prepared. The aminolysis of the latter effected by benzylamine, morpholine, piperidine, and pyrrolidine occurs in keeping with Krasusky rule to afford methyl-N-[4-(3-R-amino-2-hydroxypropoxy)phenyl]carbamates.     

Separation and determination of 4-(1,1,3,3-tetramethylbutyl)phenyl dihydrogenphosphate and di-[4-(1,1,3,3-tetramethylbutyl)phenyl] hydrogenphosphate by high-performance liquid chromatography

4-(1,1,3,3-Tetramethylbutyl)phenyl dihydrogenphosphate and di-[4-(1,1,3,3-tetramethylbutyl)phenyl] hydrogenphosphate (0.01–1 mg ml^-1) in aqueous phosphoric acid raffinates can be separated on a reversed-phase μ Bondapak C₁₈ column by gradient elution with methanol/water, and quantified at 267 nm. Raffinates are extracted with 4-methyl-2-pentanone; the two phosphates can then be determined with errors less than ±5%.