- PROCESS FOR THE PURIFICATION OF INDOLE CARBAZOLE ALKALOIDS
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Disclosed is a process for the purification of staurosporine (1), which comprises salification of staurosporine (1) (Formula (1)) by treatment with a mineral acid to give a precipitated salt, isolation of the staurosporine (1) precipitated salt, treatment of the staurosporine (1) isolated salt with an organic base, and isolation of staurosporine (1). Also disclosed are novel polymorphic forms of the mono- and bis-hydrochloride salts of staurosporine (1).
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Page/Page column 16
(2021/09/11)
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- COMPOUNDS FOR IMMUNOPOTENTIATION
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Methods of stimulating an immune response and treating patients responsive thereto with 3,4-di(1H-indol-3-yl)-1H-pyrrole-2,5-diones, staurosporine analogs, derivatized pyridazines, chromen-4-ones, indolinones, quinazolines, nucleoside analogs, and other small molecules are disclosed.
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Page/Page column 140
(2010/02/15)
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- Design and implementation of an efficient synthetic approach to pyranosylated indolocarbazoles: Total synthesis of (+)-RK286c, (+)-MLR-52, (+)-staurosporine, and (-)-TAN-1030a
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A total synthesis of the natural products (+)-staurosporine (2), (+)-RK286c (3), (-)-TAN-1030a (4), and (+)-MLR-52 (5) has been achieved. The synthetic strategy involves the stereoselective ring expansion of a furanosylated indolocarbazole [(+)-8] to a pyranosylated congener [(+)-12] that serves as a common intermediate in the production of 2-5.
- Wood, John L.,Stoltz, Brian M.,Goodman, Steven N.,Onwueme, Kenolisa
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p. 9652 - 9661
(2007/10/03)
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- Staurosporine and ent-staurosporine: The first total syntheses, prospects for a regioselective approach, and activity profiles
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The total syntheses of staurosporine and ent-staurosporine have been achieved. Both glycosidic bonds were built from glycal precursors. The first was constructed by intermolecular coupling of an indole anion with a 1,2-anhydrosugar derived from an endo-glycal by direct epoxidation. The second bond was assembled from an exo-glycal by intramolecular iodoglycosylation.
- Link,Raghavan, Subharekha,Gallant, Michel,Danishefsky, Samuel J.,Chou,Ballas, Lawrence M.
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p. 2825 - 2842
(2007/10/03)
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