Skip to main content
. Author manuscript; available in PMC: 2018 Nov 1.
Published in final edited form as: Bioorg Med Chem. 2017 Sep 19;25(21):5975–5980. doi: 10.1016/j.bmc.2017.09.022

Table 2.

Comparison between arylstannane chemistry (method A & B, see details in ESI) from the literature and our aryliodonium salts approach for the astatination of the 9E7.4 antibody.

[211At]SAB RCY (%)d Conjugation yield (%)e Overall decay corrected RCY (%) Procedure duration (min)
Method Aa 33–58f 51–61 20–30 200 ± 10
Method Bb 75–93 27–30 24–29 120 ± 10
This workc 77–84 54–60 53–57 140 ± 10
a

SAB produced from the tin precursor with N-chlorosuccinimide as oxidizing agent and purified by HPLC before conjugation (n = 2).

b

SAB produced from the tin precursor with N-iodosuccinimide as oxidizing agent and conjugated crude without purification (n = 3).

c

SAB produced from aryliodonium 4a and purified on a silica Sep-Pak Vac 3cc (500 mg) cartridge before conjugation (n = 5).

d

Decay corrected RCYs of purified [211At]SAB.

e

Conjugation yields are given after purification by gel filtration. Such purification leads typically to 20–25% loss of radiolabeled antibody on the purification column.

f

Crude RCY was typically 70–90%; major loss due to HPLC purification.