4- OR 6-SUBSTITUTED ALDOSTERONES, ITS PREPARATION AND METHOD FOR USING THE SAME IN IMMUNOASSAY

摘要

NEW MATERIAL:A substituted aldosterone of formula I [either one of R<1> and R<2> is H, R<2> is S(CH2)1-3COR<3> or OCO(CH2)1-5COR<3> when R<1> is H; R<1> is S(CH2)1-3COR<3> when R<2> is H; R<3> is OH or tyramine residue which may be iodinated, (7-aminoheptanoyl)tyrosine lower alkyl ester residue, histamine residue or histidine residue]. EXAMPLE:( 11beta, 18-Epoxy-18alpha, 21-dihydroxy-3, 20-dioxo-4-pregnen-4-ylthio )acetic acid. USE:Useful as a haptene or tracer in the immunoassay. PROCESS:A compound of formula II (X is a protecting group of the glycol) is subjected to the elimination reaction of the protecting group preferably at room temperature in an inert gas stream under acidic conditions to give the compound of formula I .