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ChemicalBook CAS DataBase List Epothilone B

Epothilone B synthesis

13synthesis methods
-

Yield:152044-54-7 71%

Reaction Conditions:

with TrisNHNH2;triethylamine in 1,2-dichloro-ethane at 50; for 6 h;

Steps:

Compound 51:

To a solution of 49 (0.7 mg, 1. [38] [UMOL)] and TrisNHNH2 (20.6 mg, 69 [UMOL)] in [C1CH2CH2CI] (0.4 [ML)] at [50 °C] was added Et3N (9. 6 μL, 69 mol). The reaction was monitored by HPTLC (hexane/EtOAc = 1/2). After stirring for 6 h, the mixture was cooled to rt, diluted with EtOAc and filtered through a pad of silica gel, which was rinsed with EtOAc. After concentrating, the residue was purified by preparative TLC (hexane/EtOAc= 1/2) gave 51 (0.5 mg, 0.985 μmol, 71%) as a white solid. The spectral data of 51 was identical to those reported of EpoB.

References:

WO2004/18478,2004,A2 Location in patent:Page 83

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