| 190778-65-5

• CAS: 190778-65-5
• 化学式: C₄₆H₆₀O₁₄Si
• 分子量: 865.059
• InChiKey: QCRBEFSCFBTKCT-RJHFICIWSA-N

反应信息

• 作为反应物：
  描述：

  在 盐酸 作用下， 以 乙腈 为溶剂， 以76%的产率得到[(1S,2S,3R,4S,7R,9S,10S,12R,15S)-4,12-diacetyloxy-15-[(2R,3S)-2,3-dihydroxy-3-phenylpropanoyl]oxy-1,9-dihydroxy-10,14,17,17-tetramethyl-11-oxo-6-oxatetracyclo[11.3.1.03,10.04,7]heptadec-13-en-2-yl] benzoate
  参考文献：
  名称：

  Structure-activity relationships study at the 3′-N position of paclitaxel-part 1: Synthesis and biological evaluation of the 3′-(t)-butylaminocarbonyloxy bearing paclitaxel analogs

  摘要：

  An efficient syntheses of the 3'-N isomeric paclitaxel analogs, 4 and 5, are described. A highly diastereoselective Sharpless asymmetric dihydroxylation reaction is utilized to establish the required (2'R, 3'S) stereochemistry on the C-13 side chain. Both of the 3'-N modified analogs 4 and 5 were found to be cytotoxic in vitro. Analog 4 also displayed comparable in vivo activity to that of paclitaxel in the ip M-109 tumor model. (C) 1997 Elsevier Science Ltd.

  DOI：

  10.1016/s0960-894x(97)10142-1
• 作为产物：
  描述：

  在 potassium osmate(VI) 、 N-甲基吲哚酮 、 Hydroquinone 1,4-phthalazinediyl diether 、 叔丁醇 作用下， 以 四氢呋喃 为溶剂， 以85%的产率得到
  参考文献：
  名称：

  Structure-activity relationships study at the 3′-N position of paclitaxel-part 1: Synthesis and biological evaluation of the 3′-(t)-butylaminocarbonyloxy bearing paclitaxel analogs

  摘要：

  An efficient syntheses of the 3'-N isomeric paclitaxel analogs, 4 and 5, are described. A highly diastereoselective Sharpless asymmetric dihydroxylation reaction is utilized to establish the required (2'R, 3'S) stereochemistry on the C-13 side chain. Both of the 3'-N modified analogs 4 and 5 were found to be cytotoxic in vitro. Analog 4 also displayed comparable in vivo activity to that of paclitaxel in the ip M-109 tumor model. (C) 1997 Elsevier Science Ltd.

  DOI：

  10.1016/s0960-894x(97)10142-1