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h series of 133 2 4 2-pyridyl)-1,2-diarylalkanols, or compounds closely related to them, were synthesized and assayed for their hypocholesteremic and estrogenic activities in rats. Many of these compounds were active in both tests, but there is no necessary correlation between the two effects. Compound 16 was selected for preclinical toxicologic study, followed by a study of its hypocholesteremic effect in man. The compound selected was remarkably nontoxic in all species studied, but it had no hypocholesteremic el'fect in the dog, the monkey, or in man.

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A-Substituted-2-mercaptoacetamidines and functional derivatives, including the corresponding disulfides, Bunte salts, and phosphorothioates, have been synthesized and found as a class to be highly effective antiradiation agents. Variations in the N substituent include alkyl, cycloalkyl, cycloalkylalkyl, aralkyl, hydroxyalkyl, cycloalkyloxyalkyl, aryloxyalkyl, thioethers, and heteroaralkyl groups. A synthesis other than the conventional ones was needed and developed for the key intermediate, A-substituted-ethyl 2chloroacetimidate salt, in which the substituent possessed a bulky carbon skeleton. Treatment of 2chloroacetamides with Meerwein's reagent gave ethyl 2-chloroacetimidate fluoroborates (VI) (Ri or R2 = H) or (2-chloro-l-ethoxyethylidene)methylammonium tetrafluoroborates (VI) (Rj and R2 H). This allowed displacement of alkoxide by NH3 rather than by a bulky amine. Half-life determinations in EtOH were made of purified samples of VI in an attempt to correlate stability with successful preparation of 2-chloroacetamidine (V). Use of 1 -amino-2-propanol in the Pinner amidine synthesis resulted in a re-