Methods for modulating lipoprotein lipase (LPL) and Apoliprotein C2 (ApoC2) expression and/or activity in the treatment of peripheral and central nervous system tissue disease states with C-6 substituted estradiol derivatives are presented herein.

The present disclosure relates to methods of carbon-carbon bond fragmentation.

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), wherein P.sup.1 and P.sup.2 are each independently a protecting group selected from R.sup.2—Si—R.sup.3R.sup.4, or R.sup.1CO—, wherein R.sup.1 is a group selected from C.sub.1-6alkyl or C.sub.3-6cycloalkyl, each group being optionally substituted by one or more substituents independently selected from fluoro or C.sub.1-4alkyl; R.sup.2, R.sup.3 and R.sup.4 are each independently a group selected from C.sub.1-6alkyl or phenyl, each group being optionally substituted by one or more substituents independently selected from fluoro or C.sub.1-4alkyl; b) reacting the compound of formula (III) in the presence of palladium acetate or a derivative thereof to produce compound of formula (IV); and c) reacting the compound of formula (IV) with a reducing agent to produce compound of formula (I). ##STR00001##

Methods for modulating lipoprotein lipase (LPL) and Apoliprotein C2 (ApoC2) expression and/or activity in the treatment of peripheral and central nervous system tissue disease states with C-6 substituted estradiol derivatives are presented herein.

The present invention relates to a method of preparing estradiol derivatives and/or estrone derivatives, which are suitable for radiolabeling. The present invention further relates to the estradiol derivatives and/or estrone derivatives, preferably obtained by the method of the present invention, as well as to the use of the estradiol derivatives and/or estrone derivatives for radiolabeling with diagnostic and/or therapeutic radionuclides. The present invention further relates to a method of imaging and/or diagnosis of breast cancer as well as to a method of treatment of breast cancer.

A process is provided for the making of estetrol starting from a 3-A-oxy-estra-1,3,5(10),15-tetraen-17-one, wherein A is an C.sub.1-C.sub.5 alkyl group, preferably a methyl group, or a C.sub.7-C.sub.12 benzylic group, preferably a benzyl group. This process is particularly suitable to industry.

Copper-catalyzed radiofluorination of iodonium salts, iodonium salts, and compounds obtained by copper-catalyzed radiofluorination of iodonium salts are disclosed. Diagnostic and therapeutic methods involving such compounds also are disclosed.

The present disclosure relates to methods of carbon-carbon bond fragmentation.

A process is provided for the making of estetrol starting from a 3-A-oxy-estra-1,3,5(10),15-tetraen-17-one, wherein A is an C.sub.1-C.sub.5 alkyl group, preferably a methyl group, or a C.sub.7-C.sub.12 benzylic group, preferably a benzyl group. This process is particularly suitable to industry.

Copper-catalyzed radiofluorination of iodonium salts, iodonium salts, and compounds obtained by copper-catalyzed radiofluorination of iodonium salts are disclosed. Diagnostic and therapeutic methods involving such compounds also are disclosed.