PROCESS FOR THE PREPARATION OF 17-DESOXY-CORTICOSTEROIDS
The present invention provides an improved process for the preparation of 17-desoxy corticosteroid derivatives in a single chemical step by reacting the 17-hydroxy starting material with an excess of Trimethylsilyl Iodide. The present invention is specifically advantageous in preparing 17-desoxy corticosteroid derivatives having one or more halogen groups at positions 2, 6, 7 or 9 of the corticosteroid such as Clocortolone or Desoximetasone.
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Page/Page column 19-20
(2012/02/05)
Isomerisation of 6beta-fluorosteroids into the corresponding 6alpha-fluoro derivatives
Described herein is the isomerisation process of 6β-fluorosteroids into the corresponding pharmacologically active 6α-fluoro derivatives, comprising the reaction of 6β-fluorosteroids, or 6α/6β isomeric mixtures, with an organic base containing a diazoimino group in a suitable organic solvent.
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(2008/06/13)
16α-methylation process
Disclosed is a process for the production of a Δ17(20) -steroid of the formula STR1 which comprises starting with a 16-unsaturated corticoid of the formula STR2 and contacting the 16-unsaturated corticoid (I) with a methylating agent in the presence of a copper catalyst and a silylating agent.
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(2008/06/13)
16α-methylatedΔ17(20)-corticoids
C16 -unsaturated corticoids are readily transformed to the corresponding 16α-methyl-17α-hydroxy corticoids by use of a Δ17 (20)-20-silyl ether.
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(2008/06/13)
Process for the preparation of 6-halo-pregnanes
The invention relates to a new process for the preparation of 6α-halo-3-keto-Δ1,4 -pregnadiene-derivatives in two-steps-synthesis affording directly 6α-halo-derivatives by reacting 3-keto-9β,11β-oxido-Δ1,4 -pregnadiene-derivatives with a suitable acylating or etherifying agent to give the corresponding new 3-enol-derivatives which are finally halogenated by using a suitable halogenating agent.
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(2008/06/13)
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