【药物名称】Ixabepilone, 16-Aza-epothilone B, BMS 247550-01, NSC-710428, BMS-247550
化学结构式(Chemical Structure):
参考文献No.46617
标题:A process for the preparation of ring-opened epothilone intermediates which are useful for the preparation of epothilone analogs
作者:Borzilleri, R.M.; Soong-Hoon, K. (Bristol-Myers Squibb Co.)
来源:WO 9927890
合成路线图解说明:

The cleavage of the lactone group of epothilone B (I) by means of Na-N3 and tetrakis triphenylphosphine palladium (0) in THF gives the azido carboxylic acid (II), which is reduced with polymer-supported PPH3 (or in solution) or with H2 over PtO2 in ethanol to yield the amino acid (III). Finally, this compound is cyclized by means of diphenylphosphoryl azide (DPPA) in DMF.

参考文献No.46618
标题:Epothilone derivs.
作者:Vite, G.D.; Kim, S.-H.; Johnson, J.A.; Borzilleri, R.M. (Bristol-Myers Squibb Co.)
来源:WO 9902514
合成路线图解说明:

The cleavage of the lactone group of epothilone B (I) by means of Na-N3 and tetrakis triphenylphosphine palladium (0) in THF gives the azido carboxylic acid (II), which is reduced with polymer-supported PPH3 (or in solution) or with H2 over PtO2 in ethanol to yield the amino acid (III). Finally, this compound is cyclized by means of diphenylphosphoryl azide (DPPA) in DMF.

参考文献No.595142
标题:A novel application of a Pd(0)-catalyzed nucleophilic substitution reaction to the regio- and stereoselective synthesis of lactam analogues of the epothilone natural products
作者:Borzilleri, R.M.; Zheng, X.; Schmidt, R.J.; et al.
来源:J Am Chem Soc 2000,122(37),8890
合成路线图解说明:

The cleavage of the lactone group of epothilone B (I) by means of Na-N3 and tetrakis triphenylphosphine palladium (0) in THF gives the azido carboxylic acid (II), which is reduced with polymer-supported PPH3 (or in solution) or with H2 over PtO2 in ethanol to yield the amino acid (III). Finally, this compound is cyclized by means of diphenylphosphoryl azide (DPPA) in DMF.

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