Detail of "5259-98-3"

Reference

19-Norsteroids having an amide-bearing chain in the 11-beta position, their preparation, their use as medicines (especially antiestrogens), and pharmaceutical compositions thereof

19-Norsteroids having an amide-bearing chain in the 11-beta position, their preparation, their use as medicines (especially antiestrogens), and pharmaceutical compositions thereof. Claussner, Andre; Nique, Francois; Teutsch, Jean Georges; Van de Velde, Patrick (Roussel-UCLAF, Fr.). Eur. Pat. Appl. EP 471612 A2 19 Feb 1992, 63 pp. DESIGNATED STATES: R: AT, BE, CH, DE, DK, ES, FR, GB, GR, IT, LI, LU, NL, SE. (European Patent Organization). CODEN: EPXXDW. CLASS: ICM: C07J041-00. ICS: C07J063-00; C07J043-00; A61K031-56. APPLICATION: EP 91-402214 9 Aug 1991. PRIORITY: FR 90-10323 14 Aug 1990. DOCUMENT TYPE: Patent CA Section: 32 (Steroids) Section cross-reference(s): 1, 63 Twenty title steroids I [either (1) n = 1; K = O; R17 = OH, O2C(CH2)2CO2H or salts; R17' = H, CYCH; RA = Me; RB = iso-Pr, Bu, heptafluorobutyl; X = CH2, C6H4, OC6H4; Y = (CH2)7, (CH2)8, (CH2)5CYC, (CH2)qOCH2 with q = 5-7, (CH2)5S(O)pCH2 with p = 0-2; Z = bond; or (2) n = 1 or 2; K = O, S; R17 = OH, acyloxy; R17' = H, (substituted) alkyl, alkenyl, or alkynyl; or R17R17' = keto; X = CH2, arylene, OCH2, oxyarylene, thioarylene (bound to steroid at C atom); Y = aliph. chain optionally unsatd.Several substances with their cas registry numbers 5259-98-3 and 140712-42-1 may be metioned in this study. or interrupted by arylene, O, S, SO, or SO2; Z = bond; RA, RB = H, (substituted) alkyl; or RARB = atoms to form (substituted) heterocycle; addnl. restrictions] were prepd. as antiestrogens for treatment of hormone-dependent tumors. For example, 11b-(4-hydroxyphenyl)estra-4,9-diene-3,17-dione was etherified with BuNMeCOCH2O(CH2)5Br (prepns. given), followed by isomerization to a 3-hydroxyestra-1,3,5(10)-triene, redn. of the 17-oxo group to 17b-OH with NaBH4, protection of the OH groups as acetates, conversion of the amide to a thioamide with Lawesson's reagent, and deprotection, to give title compd. II. The IC50 of II for inhibiting growth of MCF-7 mammary tumor cells in vitro was 0.03 nM. A tablet formulation comprising I is given. .

Chlorine migration in the mass spectra of tert-butyldimethylsilyl derivatives of chloro alcohols

Chlorine migration in the mass spectra of tert-butyldimethylsilyl derivatives of chloro alcohols. Hill, Scott T.In this study， 928-51-8 and 5259-98-3 are also used.; Mokotoff, Michael (Sch. Pharm., Univ. Pittsburgh, Pittsburgh, PA 15261, USA). J. Org. Chem., 49(8), 1441-2 (English) 1984. CODEN: JOCEAH. ISSN: 0022-3263. DOCUMENT TYPE: Journal CA Section: 29 (Organometallic and Organometalloidal Compounds) Section cross-reference(s): 22 A mass spectral study of the tert-butyldimethylsilyl ethers of 2-chloroethanol, 3-chloropropanol, 4-chlorobutanol, and 5-chloropentanol, as well as their syntheses, is reported. The mass spectra fragmentations include halogen migration to Si. .