【药物名称】tRA-96023, SB-RA-31012
化学结构式(Chemical Structure):
参考文献No.37351
标题:Taxoid reversal agents for drug-resistance in cancer chemotherapy and pharmaceutical compsns. thereof
作者:Bernacki, R.J.; Ojima, I. (State University of New York, Albany)
来源:EP 0966456; US 5811452; WO 9830553
合成路线图解说明:

The compound was prepared by esterification of the 7-hydroxyl group of 13-acetylbaccatin III (I) with 4-benzoylcinnamoyl chloride (II) in the presence of 4-dimethylaminopyridine in CH2Cl2.

合成路线图解说明:

Palladium-catalyzed coupling of 4-bromobenzophenone (I) with methyl acrylate (II) afforded 4-benzoylcinnamic ester (III), which was hydrolyzed to acid (IV) with NaOH. Condensation with taxane derivative (V) in the presence of DCC and DMAP then provided the target ester.

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