Synthesis and biological evaluation of a conformationally free seco-analogue of the immunosuppressant FR901483

Authors
Bonjoch, J Diaba, F Puigbo, G Sole, D Segarra, V Santamaria, L Beleta, J Ryder, H Palacios, JM
Citation
J. Bonjoch et al., Synthesis and biological evaluation of a conformationally free seco-analogue of the immunosuppressant FR901483, BIO MED CH, 7(12), 1999, pp. 2891-2897
Citations number
33
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY
ISSN journal
09680896 → ACNP
Volume
7
Issue
12
Year of publication
1999
Pages
2891 - 2897
Database
ISI
SICI code
0968-0896(199912)7:12<2891:SABEOA>2.0.ZU;2-1
Abstract
The synthesis of an azaspirocyclic analogue of FR901483, phosphate 2, is de scribed based on the implementation of a key 5-endo aminocyclization promot ed by iodine for direct functionalization of the 1-azaspiro[4.5]decane ring at the C-3 atom. Compound 2 has no inhibitory activity in the cell prolife ration assays reported. (C) 1999 Elsevier Science Ltd. All rights reserved.