- Method for the preparation of 6alpha-fluoro corticosteroids
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A method for producing a 6α-fluorinated corticosteroid or derivative thereof by reacting a 17-hydroxy-21-ester epoxide of Formula II with a stereoselective fluorinating agent to stereoselectively form a 21-ester-17-hydroxy 6α-fluorinated compound of Formula VII R1 can be OC(O)—Rd; R4 can be C(O)—Rd; R3 can be H or Rd. Each Rd may be the same or different and is independently selected from (C1-4)alkyl, aryl and heteroaryl. The dashed line can be a single or a double bond. R4 may be, for example, acetyl; R3 may be, for example, alpha or beta methyl; R4 may be, for example, acetate or propionate. The stereoselective fluorinating agent used in the reaction may be, for example, a fluoropyridinium or fluoroquinuclidium compound, for example, Selectfluor?.
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- Composition for the topical treatment of poison ivy and other forms of contact dermatitis
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Composition for topical administration comprising (a) a corticosteroid, and (b) a drying agent.
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- Process and intermediates for the preparation of 17 alphahydroxyprogesterones and corticoids from an enol steroid
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This invention discloses an improved process for the production of corticoids from 17α-hydroxy steroids utilizing peroxymonosulfate.
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- Process for producing 6α-fluoro-Δ1,4 -3-keto steroids
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Two processes are disclosed (one-pot and two-pot) for the transformation of a 6β-fluoro-Δ1,4 -3-keto steroid (IV) to a 6α-fluoro-Δ1,4 -3-keto steroid (VI). These processes permit the introduction of a fluorine atom at the 6α position of a Δ1,4 -3-keto steroid where previously the Δ1 double bond could not be introduced until after the 6α-fluorine atom was present. The 6α-fluoro-Δ1,4 -3-keto steroids (VI) are intermediates useful in the production of pharmacologically active steroids.
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- 3-Acetoxy-9β-11β-epoxy-dienes and the preparation of the corresponding 6α-halogen-4-ene-3-ones
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The invention relates to 3-acetoxy-9β,11β,-epoxy-pregna-1,3,5-trienes and the corresponding 3,5-dienes having the general formula 1, in which on the 1,2-position a double bond may be present and in which R3 is a hydrogen or halogen atom or a hyroxy-, acyloxy-, aroyloxy or sulphonyloxygroup; R1 and/or R2 are a hydrogen atom or a hydroxy-, aroyloxy-, acyloxy- or alkylgroup containing 1-6 carbon atoms, or in which R1 and R2 form together a 16,17-isopropylidene-dioxy group, a process for the preparation of this compounds by reacting the corresponding Δ1,4 -3-keto-pregnadienes or Δ4 -3-keto-pregnenes with isopropenylacetate and a process for their direct conversion into the corresponding 6α-halogen-substituted-pregna-1,4-diene-3-ones and pregn-4-ene-3-ones with the general formula 2 by reacting them with a positive-halogen producing agent.
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- Topical clindamycin preparations
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Disclosed is an anti-inflammatory compound, 6α,9α-di-fluoro-11β,17α,21-trihydroxy-16β-methylpregna-1,4-diene-3,20-dione 17,21-diacetate, and topical pharmaceutical formulations which include antimicrobial agents.
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- Anti-inflammatory steroid
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The disclosure covers the preparation of the compound, 6α,9α-difluoro-11β,17,21-trihydroxy-16β-methylpregna-1,4-diene-3,20-dione 17α,21-diacetate, (1) and methods and formulations for its anti-inflammatory use topically, orally and parenterally.
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