摘要:
The 17-butyrate, 17-benzoate, 17,21-methyl orthobutyrate, 17,21-methyl orthobenzoate, and 17,21-dibutyrate esters of cloprednol (6-chloro-11.beta., 17.alpha., 21-trihydroxy-pregna-1,4,6-triene-3,20-dione) are useful as topical, anti-inflammatory steroids.
摘要:
A process for the direct iodination of steroids and steroid hormones in the presence of hydrogen peroxide or chloramine-T is disclosed. The antigenicity and the specific receptor binding of directly iodinated estradiol 17-beta is identical to tritiated estradiol 17-beta.
摘要:
17.alpha.-Acyloxy-5.alpha.-pregnanes (I) and 17.alpha.-acyloxy-5.alpha.-pregnanes (IV) have an excellent activity split providing high topical anti-inflammatory activity with very low systemic side effects.
摘要:
Corticoids of the formula ##STR1## wherein X is fluorine, chlorine andR is hydrogen, C.sub.1-6 alkanoyl, benzoyl or --OCO--A--COOHwhereinA is a carbon-to-carbon bond or a C.sub.1-6 hydrocarbon chain,or whenR is --OCO--A--COOH, the physiologically acceptable salts thereof with a base,have high effectiveness, e.g., antiinflammatorily but with attendant low side effects.
摘要:
Saturated organic compounds containing a hydrogen atom bound to a tertiary carbon atom may be electrophilically fluorinated by reaction with an electrophilic fluorinating agent such as molecular fluorine or trifluoromethyl hypofluorite under conditions whereby the formation of free fluorine radicals is suppressed, e.g. by the presence of a free radical inhibitor such as oxygen or nitrobenzene, the reactants being substantially homogeneously dispersed in a liquid medium, e.g. a solvent medium such as fluorotrichloromethane or chloroform/fluorotrichloromethane, so that the said hydrogen atom is electrophilically replaced by a fluorine atom. The fluorination is highly selective and, in the case of complex substrates such as saturated steroids which contain a number of tertiary C--H bonds, may be substantially completely confined to replacement of the hydrogen atom at the tertiary carbon atom which has the highest electron density about the C--H bond. The electron density and thus the direction of the fluorination may be controlled by appropriate selection of substituent groupings in the substrate molecule.Novel 14.alpha.-fluorosteroids are also disclosed, including compounds having valuable androgenic or progestational activity and useful synthetic intermediates.
摘要:
Process for the preparation of steroids.The steroid 21-thioesters are prepared by preparing the corresponding sulphonates in acetonic suspension and by reacting this suspension directly with a thiocarboxylate.Preparation of synthesis intermediates.
摘要:
What is disclosed is corticoid 17-(alkyl carbonates) of the formula ##STR1## as defined in the specification, which compounds can be used in veterinary therapy and human therapy, in the form of suspensions, ointments, creams, sprays and the like, for the treatment of inflammatory dermatoses of very diverse cause.
摘要:
Novel steroids are described together with processes of making them and pharmaceutical compositions containing them. The steroids have pharmaceutical activity, especially anti-inflammatory activity. They are all 2-Bromo-6.beta.-fluoro-pregna-1,4-diene-3,20-diones.
摘要:
17-Keto steroids (I) in their protected form (IIa or IIb) are reacted with a metalated olefin (VI) to give a 21-aldehyde (IV) which is readily transformed to a 16-unsaturated pregnane (V) which is useful in the production of commercially important substituted corticoids.
摘要:
Steroidal [16.alpha., 17-d]cyclohexene-21-carboxylic acid esters can be prepared from 21-hydroxy-.DELTA..sup.16 -steroids by first converting the starting steroid to a 21-carboxylic acid ester -.DELTA..sup.16 -steroid and then fusing the cyclohexene ring to the 16,17-positions of the intermediate.