Preparation of 14,15-secoestra-1,3,5(10)-trien-15-ynes, inhibitors of estradiol dehydrogenase
The conversion of estrone to 14,15-secoestratrien-15-ynes, inactivators of estradiol dehydrogenase from human term placenta, is described.The optically pure precursor 7-acetoxy-octahydro-2-phenanthrenecarboxylic acid methyl ester is prepared from estrone
Auchus, Richard J.,Palmer, James O.,Carrell, H. L.,Covey, Douglas F.
PROCESS FOR THE PRODUCTION OF ESTETROL INTERMEDIATES
The present invention relates to a process for the preparation of a compound of formula (I) said process comprising the steps of : a) reacting a compound of formula (II), with an acylating or a silylating agent to produce a compound of formula (III), wher
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Page/Page column 18
(2013/02/28)
STEREOSELECTIVE REDUCTION OF ALPHA-HYDROXYKETONE
The present invention provides methods for 1, 2-asymmetric reduction of other compounds wherein 1,2- trans diol is present. In particular the present invention discloses preparation of 17β-Estriol and its derivatives having substantially free of 17α-Estriol impurity using an achiral reductant sodium triacetoxy borohydride.
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Page/Page column 8-9
(2012/03/27)
Construction of polysubstituted olefins through Ni-Catalyzed direct activation of Alkenyl C-O of substituted alkenyl acetates
(Figure Presented) Reliable companion: For the first time cross-coupling between alkenyl acetates and arylboroxines/PhZnCl has been developed via Ni catalysis. Alkenyl acetates could be well-differ-entiated from aryl acetates (see scheme). This reliable method provides a convenient pathway to construct polysubstituted styrene derivatives.