Title:
17-(3-ピリジル)ステロイドの合成
Document Type and Number:
Japanese Patent JP3722835
Kind Code:
B2
Abstract:
A method of preparing a 3 beta -hydroxy- or 3 beta -(lower acyloxy) 16,17-ene-17-(3-pyridyl)-substituted steroid, wherein the 3 beta -(lower acyloxy) group of the steroid has from 2 to 4 carbon atoms, which comprises subjecting a 3 beta -hydroxy-16,17-ene-17-iodo or -bromo steroid to a palladium complex-catalysed cross-coupling reaction with a (3-pyridyl)-substituted borane in which the pyridine ring is substituted at the 5-position by an alkyl group of 1 to 4 carbon atoms or is unsubstituted thereat, in a proportion of at least 1.0 equivalent of borane per equivalent of steroid, in an organic liquid which is a solvent for the 3 beta -hydroxy steroidal reaction product, and optionally esterifying the resulting 3 beta -hydroxy steroidal reaction product with an esterifying agent effective to replace the hydroxy group by a said lower acyloxy group, which method comprises (a) carrying out the reaction with not more than 1.2 equivalents of borane per equivalent of steroid or (b) crystallising the product of the cross-coupling reaction from a mixture of acetonitrile and methanol.
Inventors:
Potter, The Errored Andrew
Hardcastle, Ian Robert
Hardcastle, Ian Robert
Application Number:
JP51016395A
Publication Date:
November 30, 2005
Filing Date:
September 22, 1994
Export Citation:
Assignee:
Brititsushi Technology Group Limited
International Classes:
C07J13/00; C07J31/00; C07J41/00; C07J43/00; C07J51/00; (IPC1-7): C07J43/00; C07J13/00; C07J41/00
Attorney, Agent or Firm:
Yoshio Kawaguchi
Toru Nakamura
Takeshi Funayama
Toru Nakamura
Takeshi Funayama