Dey Papiya, Ajish Kumar K S, Sharma Anubha, Chattopadhyay Subrata
Bio-Organic Division, Bhabha Atomic Research Centre, Mumbai 400 085, India; Homi Bhabha National Institute, Training School Complex, Anushakti Nagar, Mumbai -400094, India.
Bio-Organic Division, Bhabha Atomic Research Centre, Mumbai 400 085, India.
Eur J Med Chem. 2018 Jan 1;143:1457-1462. doi: 10.1016/j.ejmech.2017.10.047. Epub 2017 Oct 16.
An asymmetric synthesis of a 3'-deoxy-3'-F-fluorothymidine (F-FLT) precursor has been developed wherein the deoxysugar moiety was synthesized using a novel Ga-mediated allylation of (R)-2,3-cyclohexylideneglyceraldehyde as the key step. The synthesis deviates significantly from the previous syntheses of the F-FLT precursors wherein the expensive starting material, thymidine was used.
已开发出一种3'-脱氧-3'-氟胸苷(F-FLT)前体的不对称合成方法,其中脱氧糖部分的合成以(R)-2,3-环己叉基甘油醛的新型镓介导烯丙基化为关键步骤。该合成方法与之前合成F-FLT前体的方法有显著不同,之前的方法使用了昂贵的起始原料胸苷。