【药物名称】
化学结构式(Chemical Structure):
参考文献No.647824
标题:Water-soluble, core-modified porphyrins as novel longer-wavelength-absorbing sensitizers for photodynamic therapy. II. Effects of core heteroatoms and meso-substituents on biological activity
作者:Hilmey, D.G.; Abe, M.; Nelen, M.I.; Stilts, C.E.; Baker, G.A.; Baker, S.N.; Bright, F.V.; Davies, S.R.; Gollnick, S.O.; Oseroff, A.R.; Gibson, S.L.; Hilf, R.; Detty, M.R.
来源:J Med Chem 2002,45(2),449
合成路线图解说明:

Dilithiation of thiophene (I) employing an excess of BuLi in the presence of TMEDA produced the intermediate 2,5-dilithiothiophene (II). Addition of 4-fluorobenzaldehyde (III) to the organolithium compound (II) afforded the bis-carbinol adduct (IV). Alternatively, addition of benzaldehyde (V) to (II) provided adduct (VI). Boron trifluoride-catalyzed condensation of pyrrole (VII) with diol (IV) yielded the bis(alpha-pyrrolylbenzyl)thiophene (VIII). The dithiaporphyrin derivative (IX) was then obtained by condensation between (VIII) and (VI) in the presence of boron trifluoride. Finally, aromatic sulfonation of (IX) with hot sulfuric acid, followed by neutralization with NaOH furnished the title disulfonate disodium salt.

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