Compounds having the formula

##STR00001##

or solvates of the compounds can be used as intermediates in the preparation of the synthetic steroids, Etonogestrel and Desogestrel, as well as other pharmaceutically active agents.

The present invention provides a system for evaporating a radioactive fluid, a method for the synthesis of a radiolabelled compound including this system, and a cassette for the synthesis of a radiolabelled compound comprising this system. The present invention provides advantages over known methods for evaporation of a radioactive fluid as it reduces drastically the amount of radioactive gaseous chemicals that are released in the hot cell. It is gentler and more secure compared to the known process and provides access to radiosyntheic processes that may not been acceptable for safety reasons related to release of volatile radioactive gases during evaporation. In addition, the process yields are higher because the radioactive volatiles are labelled intermediate species.

The present invention relates to a process for the preparation of a compound of formula (I) comprising the steps of a) reacting a compound of formula (II) with a silylating or an acylating agent to produce compound of formula (III), wherein P.sup.1 is a protecting group selected from R.sup.2—Si—R.sup.3R.sup.4 or R.sup.1CO—, 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) halogenation or sulfinylation of the compound of formula (III) to produce a compound of formula (IV); wherein X is halo, or —O—SO—R.sup.5, and R.sup.5 is a group selected from C.sub.6-10aryl or heteroaryl, each group being optionally substituted by one or more substituents independently selected from chloro or C.sub.1-4alkyl; c) dehalogenation or desulfinylation of the compound of formula (IV) to produce compound of formula (V); and d) reacting the compound of formula (V) with a reducing agent to produce compound of formula (I). ##STR00001##

Described herein are methods and devices that allow the generation of [F-18]triflyl fluoride and other [F-18] sulfonyl fluorides (such as [F-18]tosyl fluoride) in a manner that is suitable for radiosynthesis of F-18 labeled radiopharmaceuticals using currently available synthesis modules.

A process for the preparation of 11-methylene steroids from di-keto steroids involves selective olefination of the ketone at position 11 of the di-keto steroids. The resulting 11-methylene steroid products can be used as intermediates in the preparation of the synthetic steroids, Etonogestrel and Desogestrel, as well as other pharmaceutically active agents.

Provided herein are 3,3-disubstituted 19-nor-steroidal compounds according to Formula (I):

##STR00001##

and pharmaceutical compositions thereof. Such compounds are contemplated useful for the prevention and treatment of a variety of CNS-related conditions, for example, treatment of sleep disorders, mood disorders, schizophrenia spectrum disorders, disorders of memory and/or cognition, movement disorders, personality disorders, autism spectrum disorders, pain, traumatic brain injury, vascular diseases, substance abuse disorders and/or withdrawal syndromes, tinnitus, status epilepticus.

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 novel steroidal compounds of formula (I), process for preparation of the same and composition comprising these compounds.

##STR00001##

An estrogen receptor selective ligand can be a compound according to Structure 1:

##STR00001##

wherein m is 0, 1, or 2 and R is H, a C.sub.1 to C.sub.5 alkyl group, vinyl, CF.sub.3, CH.sub.2CH.sub.2F, CH.sub.2CHF.sub.2, or CH.sub.2CF.sub.3. A composition (e.g., pharmaceutical or cosmetic composition) can include an effective amount of a compound according to Structure 1 and a physiologically acceptable carrier, diluent, or excipient, formulated for topical administration. A method (e.g., therapeutic or cosmetic method) can include administering to a subject in need thereof an effective amount of a compound according to Structure 1 or a composition including Structure 1. Administration can be topical (e.g., to skin, scalp or mucosa).

The present invention relates to a process for the preparation of estra-1,3,5(10)-trien-3, 15a, 16a, 17-tetraol (estetr-01), via a silyl enol ether derivative 17-B-oxy-3-A-oxy-estra-1,3,5(10), 16-tetraene, wherein A is a protecting group and B is Si(R.sup.2).sub.3. The invention further relates to a process for the synthesis of 3-A-oxy-estra-1,3,5(10), 15-tetraen-17-one, in which A is a protecting group, via silyl enol ether derivative 17-B-oxy-3-A-oxy-estra-1,3,5(10),16-tetraene, and B is Si(R.sup.2).sub.3.