- A high-purity kaba he game process for the preparation of intermediate
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The invention belongs to the technical field of drug synthesis, and particularly relates to a compound (2alpha, 5beta, 7beta, 10beta, 13alpha)-4-(acetyloxy)-13-({(2R, 3S)-3-[(tert-butoxycarbonyl)amino]-2-[2-methoxy-2-prop-2-yl]oxy]-3-phenylpropionyl}oxy)-1,7,10-trimethoxy-9-oxo-5,20-epoxy-11-ene-2-yl benzoate (compound II, namely '7, 10, 13-trimethoxy-10-DAB'). The invention also relates to a preparation method of high-purity (2alpha, 5beta, 7beta, 10beta, 13alpha)-4-(acetyloxy)-13-({(2R, 3S)-3-[(tert-butoxycarbonyl)amino]-2-[2-methoxy-2-prop-2-yl]oxy]-3-phenylpropionyl}oxy)-1-hydroxy-7,10-dimethoxy-9-oxo-5,20-epoxy-11-ene-2-yl benzoate (compound 1). The preparation method comprises the steps of silica gel chromatographic column chromatography and recrystallization. In the compound I prepared by the preparation method, the content of impurities compound II and compound III is remarkably reduced. The compounds I and III can be used for preparing an anti-cancer drug cabazitaxel.
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Paragraph 0038; 0039
(2017/04/27)
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- β-lactams, methods for the preparation of taxanes, and sidechain-bearing taxanes
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Novel β-lactams finding utility as intermediates in the preparation of sidechain-bearing taxanes such as taxol and taxol derivatives. The present invention also relates to novel methods of coupling β-lactams to form such sidechain-bearing taxanes, and to novel sidechain-bearing taxanes.
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Page column 11
(2010/01/30)
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- β-lactams, methods for the preparation of taxanes, and sidechain-bearing taxanes
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Novel β-lactams finding utility as intermediates in the preparation of sidechain-bearing taxanes such as taxol and taxol derivatives. The present invention also relates to novel methods of coupling β-lactams to form such sidechain-bearing taxanes, and to
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- β-lactams, methods for the preparation of taxanes, and sidechain-bearing taxanes
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Novel β-lactams finding utility as intermediates in the preparation of sidechain-bearing taxes such as tall and tall derivatives. The present invention also relates to novel methods of coupling β-lactams to form such sidechain-bearing taxes, and to novel sidechain-bearing taxes.
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- Diastereoselective addition of grignard reagents to azetidine-23-dione: Synthesis of novel taxol analogues
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Synthesis and cytotoxicity properties of novel C-2' analogues of paclitaxel are described. The analogues were synthesized using Holton's β-lactam approach to append the side chain on baccatin III. The key intermediate to the synthesis of novel analogues w
- Kant, Joydeep,Schwartz, Wendy S.,Fairchild, Craig,Gao, Qi,Huang, Stella,Long, Byron H.,Kadow, John F.,Langley, David R.,Farina, Vittorio,Vyas, Dolatrai
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p. 6495 - 6498
(2007/10/03)
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