专利号:EP-0721461-B1 优先权日:1993-09-30 标 题 :Synthesis of 17-(3-pyridyl) steroids 发明人:POTTER GERARD ANDREW; HARDCASTLE IAN ROBERT 权利人:BTG INT LTD 摘要: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.
专利号:US-11390645-B2 优先权日:2016-08-08 标题:Process for the preparation of 3β-hydroxy-17-(1H-benzimidazol-1-YL) androsta-5,16-diene 发明人:BARBIERI FRANCESCO; LENNA ROBERTO 权利人:IND CHIMICA SRL 摘要:A process for the synthesis of β-hydroxy 3-17-(1H-benzimidazol-1-yl)androsta-5,16-diene is described, a compound also known as Galeterone and used in the treatment of prostate cancer, having the formula (6).
专利号:US-10098896-B2 优先权日:2005-03-02 标 题:C-17-heteroaryl steroidal CYP17 inhibitors/antiandrogens, in vitro biological activities, pharmacokinetics and antitumor activity 发明人:BRODIE ANGELA; NJAR VINCENT C O 权利人:THE UNIV OF MARYLAND BALTIMORE; UNIV MARYLAND 摘要:Described are steroidal C-17 benzoazoles, pyrimidinoazoles (azabenzoazoles) and diazines. Methods for their synthesis are also described, which include methods having a step of nucleophilic vinylic “addition-eliminationâ€? substitution reaction of 3β-acetoxy-17-chloro-16-formylandrosta-5,16-diene or analogs thereof and benzoazole or pyrimidinoazole nucleophiles and methods having a palladium catalyzed cross-coupling reaction of 17-iodoandrosta-5,16-dien-3β-ol or analogs thereof with tributylstannyl diazines. The compounds are potent inhibitors of human CYP17 enzyme as well as potent antagonists of both wild type and mutant androgen receptors (AR). The compounds are useful for the treatment of human prostate cancer.
专利号:WO-9509178-A1 优先权日:1993-09-30 标题 :Synthesis of 17-(3-pyridyl) steroids
专利号:RU-2749134-C1 优先权日:2016-08-08 标 题:METHOD FOR SYNTHESIS OF 3β-HYDROXY-17-(1H-BENZIMIDAZOL-1-YL)ANDROSTA-5,16-DIENE
专利号:DE-69416419-T2 优先权日:1993-09-30 标题:SYNTHESIS OF 17- (3-PYRIDYL) STEROIDS