【药物名称】
化学结构式(Chemical Structure):
参考文献No.53435
标题:Long wavelength absorbing bacteriochlorin alkyl ether analogs
作者:Pandey, R.K.; Dougherty, T.J.; Potter, W.R. (Health Research, Inc.)
来源:EP 1164136; JP 2002020389
合成路线图解说明:

Bacteriopurpurin 1 (I) was obtained from the extracts of Rhodobacter sphaeroides, enriched with bacteriochlorophyll a, by treatment with KOH/n-propanol in the presence of air. Subsequent acidification of the propanol solution of (I) produced the propyl ester (II). Opening of the anhydride ring system of (II) with n-hexylamine led to a mixture of regioisomeric amido-acid compounds, which were further converted to the respective amido-esters (III) and (IV) upon treatment with diazomethane. Repeating several times the dissolution of this mixture in THF, followed by evaporation of the solvent, gave rise to the cyclic imide (V). The keto group of (V) was then reduced to alcohol (VI) employing NaBH4 in MeOH.

合成路线图解说明:

Alcohol (VI) was converted to alkyl bromide (VII) by means of a solution of HBr in HOAc. Subsequent displacement of the bromide ion of (VII) with n-heptanol in the presence of K2CO3 furnished the title heptyl ether. Alternatively, alcohol (VI) was dehydrated to the vinyl bacteriopurpurin (VIII) by a short reflux in ortho-dichlorobenzene. Then, addition of HBr to the vinyl group, followed by treatment with heptyl alcohol, afforded the target compound.

参考文献No.647846
标题:Bacteriopurpurinimides: Highly stable and potent photosensitizers for photodynamic therapy
作者:Chen, Y.; Graham, A.; Potter, W.; Morgan, J.D.; Vaughan, L.; Bellnier, D.A.; Henderson, B.W.; Oseroff, A.; Dougherty, T.J.; Pandey, R.K.
来源:J Med Chem 2002,45(2),255
合成路线图解说明:

Bacteriopurpurin 1 (I) was obtained from the extracts of Rhodobacter sphaeroides, enriched with bacteriochlorophyll a, by treatment with KOH/n-propanol in the presence of air. Subsequent acidification of the propanol solution of (I) produced the propyl ester (II). Opening of the anhydride ring system of (II) with n-hexylamine led to a mixture of regioisomeric amido-acid compounds, which were further converted to the respective amido-esters (III) and (IV) upon treatment with diazomethane. Repeating several times the dissolution of this mixture in THF, followed by evaporation of the solvent, gave rise to the cyclic imide (V). The keto group of (V) was then reduced to alcohol (VI) employing NaBH4 in MeOH.

合成路线图解说明:

Alcohol (VI) was converted to alkyl bromide (VII) by means of a solution of HBr in HOAc. Subsequent displacement of the bromide ion of (VII) with n-heptanol in the presence of K2CO3 furnished the title heptyl ether. Alternatively, alcohol (VI) was dehydrated to the vinyl bacteriopurpurin (VIII) by a short reflux in ortho-dichlorobenzene. Then, addition of HBr to the vinyl group, followed by treatment with heptyl alcohol, afforded the target compound.

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