Michel Vilkas

A Convenient Laboratory Preparation of N,N-Dimethyl-dichloro-methylene-iminium Chloride (Phosgene-iminium chloride)

Abstract A method of preparation of the title compound 1a avoiding the use of gaseous chlorine is described. Tetramethylthiuram disulfide 4 is oxidized with sulfuryl chloride to dime thyl thiocarbamoyl chloride 5, which is converted to 1a by means of phosphorus pentachloride.

Synthesis and properties of some new 3-substituted hexestrol derivatives

Abstract A series of new monosubstituted hexestrol derivatives were synthesized and the estrogenic and cytotoxic properties of some of them were studied. 3-Acetoxymethyl-hexestrol 8 has a binding affinity for the cytoplasmic estrogen receptor as high as estradiol. It is 100–1000 times lower for the coumarinic derivatives 13, 14 and 15. None of these compounds becomes covalently bound to the receptor. They display a 20–1000 times lower affinity for the estrogen receptor in the whole cell test on the MCF-7 mammary tumor cell culture. At low concentrations (10−8 M) the three coumarinic derivatives stimulate the growth of these cells (estrogenic effect) as strongly as estradiol does.