REAGENTS FOR THE ASSAY OF CARDIAC GLYCOSIDES

摘要

1441253 Oxazepinyl steroids WELLCOME FOUNDATION Ltd 21 June 1973 [22 June 1972 30 Nov 1972] 29279/72 and 55349/72 Heading C2U [Also in Division G1] The invention comprises compounds of formula wherein b is 0, 1 or 2; A is a direct bond or an optionally substituted alkylene group; RSP1/SP and RSP2/SP are each H or OH, at least one being H; Y and YSP1/SP are both H or both OH; and XSP1/SP and XSP2/SP are each H or an iodine radioisotope (e.g. SP123/SPI, SP124/SPI, SP125/SPI, SP126/SPI, SP128/SPI, SP129/SPI, SP130/SPI, SP131/SPI or SP132/SPI) provided that when Y=YSP1/SP=OH then XSP1/SP=XSP2/SP= H. Compounds VIII are prepared from the corresponding mono-, di- and tridigitoxosides by oxidative cleavage of the terminal sugar moiety (e.g. with Pb(OAc) 4 or NaIO 4 ) to give dialdehydes, reaction of which with HO-C 6 H 4 -A-NH 2 yields VIII (XSP1/SP=XSP2/SP=H; YSP1/SP=YSP2/SP=OH), reduction of which (e.g. with KBH 4 , NaBH 4 , LiBH 4 or LiAlH 4 ) yields VIII with possible reduction also of reducible substituents in A), which may then be radioiodinated, e.g. using sodium radioiodide with chloramine T. Compounds VIII containing radioiodine are used as antigens in the radioimmunoassay of cardenolide glycosides (see Division G1).