REAGENTS FOR THE ASSAY OF CARDENOLIDE GLYCOSIDES AND AGLYCONES

摘要

1441101 Cardenolide oximes WELLCOME FOUNDATION Ltd 21 June 1973 [22 June 1972] 29280/72 Heading C2U [Also in Division G1] The invention comprises compounds of formula wherein RSP1/SP-RSP5/SP are each H or OH, at least four being H, and the α-configuration being permitted to RSP2/SP only when RSP1/SP-RSP5/SP are all H; B is alkylene; Z is OH or a group of formula wherein R is H or C 1-4 alkyl; A is a direct bond or an optionally substituted alkylene group; 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. Compounds IX are prepared from the corresponding 3α- or 3#-ols by the successive steps of (a) oxidation to the 3-ones, e.g. with chromic acid, KHnO 4 or O 2 /Pt; (b) reaction with H 2 N-O-B-CO 2 H to give IX (Z=OH); (c) reaction with R-NH-A-C 6 H 4 -OH to give IX (Z=formula X; XSP1/SP=XSP2/SP=H); (d) radioiodination, e.g. using sodium radio-iodide with chloramine T. Compounds IX containing radioiodine are used as antigens in the radioimmunoassay of cardenolde glycosides and aglycones (see Division G1).