C9-imino and C10-amino derivatives of ascomycin (21-ethyl-FK 506)
✍ Scribed by Peter Nussbaumer; Maximilian Grassberger; Gerhard Schulz
- Publisher
- Elsevier Science
- Year
- 1992
- Tongue
- French
- Weight
- 132 KB
- Volume
- 33
- Category
- Article
- ISSN
- 0040-4039
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✦ Synopsis
Treatment of Ascomycin (21-ethyl-PR 506) with ammonia in alcoholic solution yields! C9-imine 5 and ClO-amine 6, whereas methylamine gives only C9-methylimine 10. lo improve the pharmacological qualities of the immunosuppressant PR 506l (1) chemical derivatization of the natural product or of the related macrolides Ascomycin' (2) and Rspamycin3 is persued worldwide. We report on a simple one step conversion of 2 into derive t ives with C9-imine or ClO-amine functionalities 4 without the use of protection/ deprotection protocols. Characteristics of their Nt4R spectra are briefly discussed.