Published March 1996
| Version v1
Journal article
Synthesis of I-125 labeled photoaffinity rapamycin analogs
- 1. SmithKline Beecham Pharmaceuticals, King of Prussia, PA (United States)
Description
Two no-carrier-added 125I-labelled photoaffinity rapamycin analogs were prepared: 7-demethoxy-7-(4-azido-3-125I-benzyloxy) rapamycin and its C28-C29 seco analog. The key reactions of the synthesis were substitution of the C7 methoxyl of rapamycin with 4-azido-3-tributylstannylbenzyloxy group, exchange of tributyltin with 125I using Na125I and Chloramine-T, and a ZnCl2 mediated retro-Aldol cleavage of the C28-C29 bond of rapamycin. (author)
Additional details
Publishing Information
- Journal Title
- Journal of Labelled Compounds and Radiopharmaceuticals
- Journal Volume
- 38
- Journal Issue
- 3
- Journal Page Range
- p. 227-237.
- ISSN
- 0362-4803
- CODEN
- JLCRD4
INIS
- Country of Publication
- United Kingdom
- Country of Input or Organization
- United Kingdom
- INIS RN
- 28011897
- Subject category
- S38: RADIATION CHEMISTRY, RADIOCHEMISTRY AND NUCLEAR CHEMISTRY;
- Descriptors DEI
- ANTIMICROBIAL AGENTS; AZIDO COMPOUNDS; CHEMICAL PREPARATION; IMMUNOSUPPRESSIVE DRUGS; IODINE 125; LABELLING; RADIOPHARMACEUTICALS
- Descriptors DEC
- ANTI-INFECTIVE AGENTS; BETA DECAY RADIOISOTOPES; DAYS LIVING RADIOISOTOPES; DRUGS; ELECTRON CAPTURE RADIOISOTOPES; INTERMEDIATE MASS NUCLEI; INTERNAL CONVERSION RADIOISOTOPES; IODINE ISOTOPES; ISOTOPES; LABELLED COMPOUNDS; MATERIALS; NUCLEI; ODD-EVEN NUCLEI; ORGANIC COMPOUNDS; ORGANIC NITROGEN COMPOUNDS; RADIOACTIVE MATERIALS; RADIOISOTOPES; SYNTHESIS