Sicor Societa 'italiana Corticosteroidi S.p.a.

Prochem Establishment

Sterosynt Ltd.

Peter MacDonald

Gaetano Palladino

Ettore Bigatti

An improved process for the preparation of doxorubicin, by means of hydrolysis of a doxorubicin ester of a dicarboxylic acid, in acid medium.

Process for the conversion of daunorubicin into doxorubicin

A compound exhibiting anti-inflammatory properties having the formula ##STR1## in which X is H, Hal or CH.sub.3 COO--; R.sub.1 is CH.sub.3 (CH.sub.2).sub.2 CH--; and R.sub.2 and R.sub.3 are separately H or Hal; and a pharmaceutical composition containing the same.

16,17 acetals of pregnane derivatives and pharmaceutical compositions

A process for the preparation of 16,17 acetals of pregnane derivatives by trans-ketalization of 16,17-acetonides is described. In the instance of the preparation of 16.alpha.,17.alpha.-butylidenedioxy-11.beta.,21-dihydroxypregna-1,4-diene- 3,20-dione, a compound having useful therapeutic properties, known also as budesonide, it is possible to obtain the more active epimer with high selectivity and remarkable economic advantages in comparison with the known methods. New 16,17 acetals of pregnane derivatives, which can be prepared by the method of the invention, are also described.

Process for the preparation of 16,17 acetals of pregnane derivatives

Novel 6.alpha.-fluoro-9.alpha.-chloro-16.beta.-methyl-prednisolone 17, 21-diesters, and a method for their preparation, are described. The novel products are particularly valuable as anti-inflammatory agents.

6.alpha.-Fluoro-9.alpha.-chloro-prednisolone 17,21-diesters

The invention relates to 3-acetoxy-9.beta.,11.beta.,-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 R.sub.3 is a hydrogen or halogen atom or a hyroxy-, acyloxy-, aroyloxy or sulphonyloxygroup; R.sub.1 and/or R.sub.2 are a hydrogen atom or a hydroxy-, aroyloxy-, acyloxy- or alkylgroup containing 1-6 carbon atoms, or in which R.sub.1 and R.sub.2 form together a 16,17-isopropylidene-dioxy group, a process for the preparation of this compounds by reacting the corresponding .DELTA..sup.1,4 -3-keto-pregnadienes or .DELTA..sup.4 -3-keto-pregnenes with isopropenylacetate and a process for their direct conversion into the corresponding 6.alpha.-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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Arese, Italy

Peter MacDonald