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Synthesis and bioactivity of photolabile sirolimus (rapamycin) analogs

✍ Scribed by Yanqui Chen; Koji Nakanishi; Diana Merrill; Chee P. Eng; Katherine L. Molnar-Kimber; Amedeo Failli; Thomas J. Caggiano

Book ID
108038848
Publisher
Elsevier Science
Year
1995
Tongue
English
Weight
199 KB
Volume
5
Category
Article
ISSN
0960-894X

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Two no-carrier-added 125I-labeled photoaffinity raparnycin analogs were prepared: 7-demethoxy-7-(4-azido-3-~~~l-benzyloxy)rapamycin (2) and its C28-C29 seco analog 3 . The key reactions of the synthesis were substitution of the C7 methoxyl of rapamycin (1) with 4-azido-3-tributylstannylbenzyloxy gro