- Studies in Antifertility Agents. 50. Stereoselective Binding of d- and l-Centchromans to Estrogen Receptors and Their Antifertility Activity
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Centchroman -7-methoxychroman hydrochloride>, an antifertility agent under clinical evaluation, has been resolved into its optical enantiomers.The cytosol estrogen receptor binding affinity and estrogenic, antiestrogenic and antiimplantation activities of the two enantiomers have been determined.The enantiomers display a 7-fold difference in receptor affinity, and a corresponding difference in stimulation of the uterine growth and antiimplantation activity was observed in rats.
- Salman, M.,Ray, Suprabhat,Anand, Nitya,Agarwal, A. K.,Singh, M. M.,et al.
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- AN IMPROVED PROCESS FOR THE PREPARATION OF TRANS 3,4- DIARYLCHROMAN AND THEIR DERIVATIVES
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The invention describes an improved and advantageous process of preparation of trans 3,4-diarylchroman and similar derivatives there of, useful as anti-fertility, anti-osteoporotic and breast cancer drugs. Condensation of arenes with 2,2- dialkyl-3-aryl c
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Page/Page column 14-15
(2009/07/18)
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- Process for the preparation of (-)-3,4-trans-diarylchromans
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Disclosed is a process for preparing (-)-3,4-trans-diarylchromans of formula I STR1 wherein R1, R2, R3, R4 and R5 are as defined in the specification. This process involves reacting a (+,-)-3,4-cis-diarylchroman with a chiral acid in an inert organic solvent to obtain the chiral acid salt of the (-)-3,4-cis enantiomer in crystalline form, subjecting the crystalline salt to hydrolysis, and rearranging the (-)-3,4-cis enantiomer to the (-)-3,4-trans enantiomer with a strong base in an inert aprotic solvent.
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