68266-31-9Relevant academic research and scientific papers
PROCESS FOR THE PREPARATION OF L-PHENYL-3-DIMETHYLAMINOPROPANE DERIVATIVES
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, (2011/08/21)
The present invention provides a process for the preparation of 1-phenyl-3-dimethylaminopropane derivatives of formula I, and its pharmaceutically acceptable salts thereof from intermediate of formula II, wherein R1 can be selected from -OR2, halo, -CH2OR2, -SR2, SOR2, SO2R2, -SO3H, -NO2, -NR2R2', - CONR2R2 ', carboxylic esters, sulfonate esters or phosphate esters and the like; R ' can be selected from hydrogen, alkyl, aryl, aralkyl, alkaryl, heteroaryl, and the like; or OR ' can be selected from -NR2R2 '; or R2 and R2 ' can be same or different and can be selected from hydrogen, alkyl, aryl, aralkyl, heteroaryl,-OR3, - COR3, -PO3(R3R4) wherein R3 and R4 can be same or different and can be selected from alkyl, aryl, aralkyl, heteroaryl and the like.
Potential Antiestrogens. Synthesis and Evaluation of Mammary Tumor Inhibiting Activity of 1,2-Dialkyl-1,2-bis(3'-hydroxyphenyl)ethanes
Hartmann, Rolf W.,Buchborn, Helga,Kranzfelder, Gerhard,Schoenenberger, Helmut,Bogden, Arthur
, p. 1192 - 1197 (2007/10/02)
The syntheses of the meso-1,2-dialkyl-1,2-bis(3'-hydroxyphenyl)ethanes and of d,l-3,4-bis(3'-hydroxyphenyl)hexane (21) are described.In vitro these compounds inhibited the estradiol receptor interaction competitively, exhibiting Ka values between 0.20*109 (20) and 0.11*106 M-1 (24).In vivo the meso compounds reduced the estrone-stimulated mouse uterine growth; the most effective compounds were 20, 22, and 23 (53, 50, and 45percent inhibition, respectively).Compounds 20 and 22-24 showed weak estrogenic activity in the mouse uterine weight test and in the vaginal cornification test.Compounds 19 (NSC-297169), 20 (NSC-297170), and 22 (NSC-297171) exhibited a dose-dependent growth inhibition on the MCF-7 human breast tumor cell line (10-6 to 10-9 M).These compounds also showed a marked dose-dependent inhibition on the DMBA-induced, hormone-dependent mammary carcinoma of the Sprague-Dawley rat corresponding to their association constants.
