Radioactive nuclide labeled propiophenone compounds

Organic compounds -- part of the class 532-570 series – Organic compounds – Amino nitrogen containing

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23230B, 424 1, 424 12, C07C 25024, C07C10330, C07G 700, G01N 3354

Patent

active

043551793

ABSTRACT:
A radioimmunoassay procedure has been discovered for bupropion [(.+-.)-2-t-butylamino-3-chloropropiophenone], an antidepressant compound, in biological fluids. Novel compounds of formula ##STR1## wherein either R.sub.2 is oxygen and R.sub.1 is (CH.sub.2).sub.n --O--(CO).sub.m --(CH.sub.2).sub.p --COOH where n is an integer from 0 to 5, m is 0 or 1, and p is an integer from 1 to 4; or R.sub.1 is hydrogen and R.sub.2 is N--O--(CH.sub.2).sub.q --COOH where q is an integer from 1 to 3, and novel methods of making them and novel intermediates useful therein are disclosed. Novel immunogens for raising bupropion specific antisera, and novel methods of making them are disclosed comprising conjugates of the novel compounds and suitable carrier material. The drug is added to the antisera together with novel radiolabeled competitor of formula ##STR2## wherein R' is a suitable radioisotope as described above and R.sub.3 is hydrogen, R.sub.4 is Cl, and R.sub.5 is oxygen, or

REFERENCES:
patent: 1926952 (1933-09-01), Legerlotz
patent: 3278600 (1966-10-01), L'Italien
patent: 3951978 (1976-04-01), Manghisi et al.
patent: 4041076 (1977-08-01), Avenia
patent: 4131686 (1978-12-01), Ikezaki et al.
Findlay et al., Res. Comm. Chem. Pathol. Pharmacol., 17(4), 595-603 (1977).

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