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filingDate 1970-04-23-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationDate 1973-05-09-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber GB-1316663-A
titleOfInvention 2-chloro-delta1,4-steroids and intermediates therefor
abstract 1316663 2-Chloro-steroids SCHERING AG 23 April 1970 [23 April 1969 (2) 19 June 1969] 19534/70 Heading C2U Novel steroids of the formula (wherein R 1 is H or CH 3 , R 2 is H, OH or Oacyl, X is F, Cl or CH 3 , Y is H or a halogen, and Z is a halogen of atomic weight equal to or less than that of Y when a halogen, or Z is #-OH, or, when Y is H, it may also be α-OH) are prepared by adding chlorine onto steroids of the formula (wherein R<SP>1</SP> 2 is as R 2 but is not OH) and either separating the resulting mixture of 1,2-dichloro- #<SP>4</SP>- and 2 - chloro - #<SP>1,4</SP> - steroids chromatographically or converting the former to the latter. Products of the formula (wherein Z<SP>1</SP> is OH and -B-A- is or -CHCl-CHCl-) may be dehydrated to the corresponding #<SP>9(11)</SP>-compounds with simultaneous elimination of HCl from the 1,2-position when -B-A- is -CHCl-CHCl-, and there converted to 9,11-dihalo compounds by addition of halogen or to the 9-halo-11#-ols by addition of HOCl or HOBr, or, via the lastnamed and the 9,11#-epoxides, into the 9α- fluoro-11#-ols. 21-Esters may be hydrolysed and the free ols acylated. Novel intermediates have the formula (wherein X and R 1 are as defined above and R 2 is H or Oacyl) or are 6α-fluoro-2-chloro-21- acetoxy - 16α - methyl - #<SP>1,4,9(11)</SP> - pregnatriene- 3,20-dione and the corresponding 9,11#-epoxide. The novel anti-inflammatory steroids of the first general formula above may be made up into pharmaceutical compositions with suitable carriers. Reference has been directed by the Comptroller to Specification 1,245,292.
priorityDate 1969-04-23-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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Total number of triples: 29.