Selective substitution of 31/42-OH in rapamycin guided by an in situ IR technique.
Molecules
; 19(6): 7770-84, 2014 Jun 10.
Article
en En
| MEDLINE
| ID: mdl-24918544
ABSTRACT
An in situ IR technique was applied in the selective synthesis of the key intermediate for rapamycin derivatives, which made the reaction endpoint easily defined. This technology solved a bothersome problem in the preparation of rapamycin derivatives, and based on this technique, the 31-OH and 42-OH of rapamycin were chemically modified by a series of quaternary ammonium salts to generate 11 compounds. The solubility of all these compounds was remarkably improved (25,000 times higher than that of rapamycin) and their structures were confirmed by MS, IR, 1D and 2D NMR techniques.
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1
Bases de datos:
MEDLINE
Asunto principal:
Sirolimus
Idioma:
En
Revista:
Molecules
Asunto de la revista:
BIOLOGIA
Año:
2014
Tipo del documento:
Article
País de afiliación:
China