The present application describes process for preparing an ortho-allylated hydroxy aryl compounds such as compounds of Formula (I) by reacting an allylic alcohol with a hydroxy aryl compound in the presence of aluminum compound selected from alumina and aluminum alkoxides and in a non-protic solvent wherein at least one carbon atom ortho to the hydroxy group in the hydroxy aryl compound is unsubstituted. The present application also includes compounds of Formula (I).

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The present invention identifies new steroidal analogues of formestane synthesized through biotransformation with significant aromatase inhibitory activity, and thus can serve as possible safe, effective, and selective anti-cancer agent towards estrogen-responsive (ER+) breast cancer. Four new derivatives of anticancer drug formestane (1), 4α,5α,7α-trihydroxyandrostane-3,17-dione (2), 3β,7β-dihydroxyandrostane-4,17-dione (3), 3β,5α,7β-trihydroxyandrostane-4,17-dione (4), and 4,11α-dihydroxyandrosta-1,4-diene-3,17-dione (5) were synthesized through bio-catalyzed structural modifications by Cunninghamella. blakesleeana and Fusarium lini. The new derivatives showed varying degree of inhibition of aromatase enzyme. Metabolite 4 (IC.sub.50=0.386±0.072 μM), showed a significant inhibitory potential, comparable to substrate 1 (IC.sub.50=0.335±0.011 μM) and standard aromatase inhibitory anti-cancer drug exemestane (IC.sub.50=0.232±0.031 μM). Metabolites 3 (IC.sub.50=1.37±0.029 μM), and 2 (IC.sub.50=5.229±0.094 μM) showed significant inhibition, while metabolite 5 (IC.sub.50=34.27±0.532 μM) showed a weak inhibitory activity as compared to standard.

The invention discloses a method for fluoroalkylation of enamines with a fluoro alkyl halide in the presence of a base.

Chiral polyvinylpyrrolidinone (CSPVP), complexes of CSPVP with a core species, such as a bimetallic nanocluster catalyst, and enantioselective oxidation reactions utilizing such complexes are disclosed. The catalytic complexes have exhibited the ability to achieve reaction products have a very high degree of optical purifies. These reaction products can be used as reagents in the synthesis of complex organic molecules, such as bioactive products, and C—H bond oxidation of complex molecules including various drugs and natural products.

Chiral polyvinylpyrrolidinone (CSPVP), complexes of CSPVP with a core species, such as a bimetallic nanocluster catalyst, and enantioselective oxidation reactions utilizing such complexes are disclosed. The catalytic complexes have exhibited the ability to achieve reaction products have a very high degree of optical purifies. These reaction products can be used as reagents in the synthesis of complex organic molecules, such as bioactive products, and C—H bond oxidation of complex molecules including various drugs and natural products.

The present invention relates to a method for preparing 7α-methyl-19-aldehyde-4-androstene-3,17-dione by electrocatalytic oxidation. The method specifically includes: adopting an H-shaped electrolytic cell for reaction, in an anode chamber, using a metal oxide catalyst as a working electrode, using 7α-methyl-17,19-dihydroxy-4-androstene-3-one as a reaction substrate, and dissolving it in a mixed solvent to be used as an anolyte, and adding nitroxide radicals to be used as a medium; and in a cathode chamber, using a platinum sheet as a counter electrode, using a weakly alkaline solution as a catholyte, carrying out an electrocatalytic oxidation reaction in a constant temperature water bath, adding an organic solvent at the end of the reaction for extraction to obtain an organic extract liquor, and taking an organic layer and carrying out distilling under a reduced pressure to obtain 7α-methyl-19-aldehyde-4-androstene-3,17-dione.

The present invention relates to compounds and their uses, in particular, compounds in the form of prodrugs that pro mote transport of a pharmaceutical agent to the lymphatic system and subsequently enhance release of the parent drug.

The invention discloses a method for fluoroalkylation of enamines with a fluoro alkyl halide in the presence of a base.

A drug delivery system for oral administration of hydrophobic drugs with enhanced and extended absorption and improved pharmacokinetics is provided. In one embodiment, formulations comprising testosterone and testosterone esters, e.g., testosterone palmitate, are disclosed. Methods of treating a hormone deficiency or effecting male contraception with the inventive formulations are also provided.

A drug delivery system for oral administration of hydrophobic drugs with enhanced and extended absorption and improved pharmacokinetics is provided. In one embodiment, formulations comprising testosterone and testosterone esters, e.g., testosterone palmitate, are disclosed. Methods of treating a hormone deficiency or effecting male contraception with the inventive formulations are also provided.