【药物名称】ER-127528
化学结构式(Chemical Structure):
参考文献No.44846
标题:Fluorides of 4-substd. piperidine derivs.
作者:Sugimoto, H.; Yamanishi, Y.; Shibata, T.; Kosaka, T.; Suzuki, E.; Takeuchi, Y.; Imura, Y. (Eisai Co., Ltd.)
来源:EP 1157989; JP 2000319258; WO 0051985
合成路线图解说明:

The lithium enolate of the indanone derivative (I) is fluorinated by treatment with N-fluorobenzenesulfonimide, to afford the corresponding fluoro ketone, which is finally isolated as the corresponding hydrochloride salt.

参考文献No.613181
标题:Recent advances in the study of acetylcholinesterase inhibitor "donepezil" (1): Synthesis and structure-activity relationships of fluorine-introduced donepezil and related compounds
作者:Takeuchi, Y.; Yamanishi, Y.; Sugimoto, H.; Suzuki, N.; Iimura, Y.; Kawakami, Y.; Inoue, A.; Kuriya, Y.; Kosasa, T.
来源:221st ACS Natl Meet (April 1 2001, San Diego) 2001,Abst MEDI 67
合成路线图解说明:

The title compound is also prepared by a related method. Indanone (I) is fluorinated by means of N-fluorobenzenesulfonimide in the presence of lithium hexamethyldisilazide, to afford the corresponding fluoro ketone (II). Subsequent dealkylation of the N-benzyl group of (II) is accomplished by treatment with 1-chloroethyl chloroformate, to produce the intermediate carbamate (III), which is then decarboxylated to the secondary amine (IV) in boiling MeOH. Finally, piperidine (IV) is reductively alkylated with 3-fluorobenzaldehyde (V) in the presence of NaBH(OAc)3.

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