US4826672A
Expired / Lapsed
US
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Astatinated organic compounds
Assignee: Harvard University
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Filing: 1985-06-07
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Granted: 1989-05-02
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Expires: 2005-06-07
Abstract
Abstract Methods and kits for incorporating a radioactive astatine isotope (particularly 211 At) into an organic compound by electrophilic astatodestannylation of organostannanes.
Inventors
- 👤 Richard A. Milius
- 👤 Richard M. Lambrecht
- 👤 William D. Bloomer
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-23 21:28
CPC Classifications
G; G01; G01N; G01N33/00; G01N33/48; G01N33/50; G01N33/58; G01N33/60; A; A61; A61K; A61K51/00; A61K51/02; A61K51/04; A61K51/0404; A61K51/0406; A61K51/0491; A61K51/08; A61K51/10; A61K51/1093; C; C07; C07C; C07C217/00; C07C217/02; C07C217/04; C07C217/06; C07C217/14; C07C217/18; C07C217/20; A61K2121/00
Claims Analysis
Total Claims: 29
Claim 1
Independent Claim
69 words
A method of making the compound At-Z where Z comprises an unsaturated organic component, and At is a radioactive isotope of astatine, said method comprising, providing a source of At + ; and reacting said At + with the compound ##STR1## to form At--Z, where R 1 , R 2 , and R 3 , are each independently selected from aryl and alkyl groups having less than 10 carbons.
Claim 2
Independent Claim
69 words
A method of making the compound At-Z where Z comprises an unsaturated organic component, and At is a radioactive isotope of astatine, said method comprising, providing a source of At + ; and reacting said At + with the compound ##STR1## to form At--Z, where R 1 , R 2 , and R 3 , are each independently selected from aryl and alkyl groups having less than 10 carbons.
Claim 3
Dependent Claim
23 words
The method of claim 1 wherein Z comprises a cell-specific binding agent or an unsaturated organic linker to a cell specific binding agent.
Claim 4
Dependent Claim
17 words
The method of claim 1 wherein said reaction is conducted in the presence of an electronegative carrier
Claim 5
Dependent Claim
20 words
The method of claim 3 wherein said electronegative carrier is Cl - , Br - , or I - .
Claim 6
Dependent Claim
19 words
The method of claim 1 wherein said method further comprises generating At 30 by oxidation of At - .
Claim 7
Dependent Claim
23 words
The method of claim 5 wherein said At - is 211 At - supplied in a concentration of less than 10 -6 M.
Claim 8
Dependent Claim
36 words
The method of claim 1 wherein R 1 , R 2 , R 3 are each independently selected from alkyl groups or substituted alkyl groups of C 5 or less and phenyl or substituted phenyl groups.
Claim 9
Dependent Claim
11 words
The method of claim 1 wherein Z is a steroidal group.
Claim 10
Dependent Claim
19 words
The method of claim 1 wherein Z is an aryl group, a substituted aryl group, or a vinyl group.
Claim 11
Dependent Claim
16 words
The method of claim 9 wherein Z comprises an aryl group capable of coupling with antibodies.
Claim 12
Dependent Claim
22 words
The method of claim 10 where Z comprises an aromatic carboxylic acid, an aromatic amine, an aromatic isocyanate, or an aromatic isothio-cyanate.
Claim 13
Dependent Claim
17 words
The method of claim 11, wherein Z is a benzoic acid or a substituted benzoic acid group.
Claim 14
Dependent Claim
15 words
The method of claim 1 wherein Z is a tamoxifen group or a vinylestradiol group.
Claim 15
Dependent Claim
42 words
A kit for performing the method of claim 1 comprising: a source of At - , an oxidizing agent capable of converting At - to At + , and a source of said R 1 --, R 2 --, R 3 --Sn--Z.
Claim 16
Dependent Claim
22 words
The kit of claim 14 wherein Z comprises a cell-specific binding agent or an unsaturated organic linker to a cell-specific binding agent.
Claim 17
Dependent Claim
14 words
The kit of claim 14 wherein said kit further comprises an electronegative carrier species.
Claim 18
Dependent Claim
19 words
The kit of claim 16 wherein said carrier is Cl - , Br - , or I - .
Claim 19
Dependent Claim
22 words
The kit of claim 14 wherein said At. is 211 At - supplied in a concentration of less than 10 -6 M.
Claim 20
Dependent Claim
37 words
The kit of claim 14 wherein R 1 , R 2 , and R 3 are each independently selected from alkyl groups or substituted alkyl groups of C 5 or less and phenyl or substituted phenyl groups.
Claim 21
Dependent Claim
11 words
The kit of claim 14 wherein Z is a steroidal group.
Claim 22
Dependent Claim
19 words
The kit of claim 14 wherein Z comprises an aryl group, a substituted aryl group, or a vinyl group.
Claim 23
Dependent Claim
16 words
The kit of claim 21 wherein Z comprises an aryl group capable of coupling with antibodies.
Claim 24
Dependent Claim
22 words
The kit of claim 22 where Z comprises an aromatic carboxylic acid, an aromatic amine, an aromatic isocyanate, or an aromatic isothio-cyanate.
Claim 25
Dependent Claim
17 words
The kit of claim 23 wherein Z is a benzoic acid or a substituted benzoic acid group.
Claim 26
Dependent Claim
15 words
The kit of claim 14 wherein Z is a tamoxifen group or a vinylestradiol group.
Claim 27
Dependent Claim
28 words
A method of making a cell-selective astatinated compound comprising producting At--Z by the method of claim 2 and reacting At--Z with a cell selective molecule comprising a polypeptide.
Claim 28
Dependent Claim
23 words
The method of claim 26 wherein said cell-selective molecule is an antibody or a protein that is specific for a cell surface receptor.
Claim 29
Dependent Claim
23 words
A kit for performing the method of claim 26 comprising: a source of At--Z or materials for making At--Z, and said cell-selective molecule.
References Cited (Backward Citations)
US4311688A
Cited
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