【药物名称】Pimecrolimus, ASM-998, ASM-981, SDZ-ASM-981, Elidel
化学结构式(Chemical Structure):
参考文献No.4686
标题:Tricyclo cpds., a process for their production and pharmaceutical compsn. containing the same
作者:Okuhara, M.; Tanaka, H.; Goto, T.; Kino, T.; Hatanaka, H. (Fujisawa Pharmaceutical Co., Ltd.)
来源:AU 8550596; EP 0184162; JP 1991072483; JP 1991072484; JP 1995224066; JP 1999012281; JP 1999343294; US 4894366; US 4929611; US 4956352; US 5110811; US 5254562; US 5266692; US 5565559
合成路线图解说明:

The silylation of the known compound FK-520 by means of tert-butyldimethylsilyl chloride (TBDMS-Cl) and imidazole in DMF gives the disilylated compound (II), which is selectively monodesilylated by means of 40% HF in acetonitrile for 2 h at 0 C yielding the monosilylated compound (III). The chlorination of (III) by means of triphenylphosphine in refluxing CCl4 gives the chloro derivative (IV), which is finally desilylated with 40% HF in acetonitrile at room temperature.

参考文献No.14821
标题:Heteroatoms-containing tricyclic cpds
作者:Baumann, K.; Emmer, G. (Novartis AG; Novartis Deutschland GmbH)
来源:AU 9165843; EP 0427680; JP 1991223291; US 5352671; US 5912238
合成路线图解说明:

The silylation of the known compound FK-520 by means of tert-butyldimethylsilyl chloride (TBDMS-Cl) and imidazole in DMF gives the disilylated compound (II), which is selectively monodesilylated by means of 40% HF in acetonitrile for 2 h at 0 C yielding the monosilylated compound (III). The chlorination of (III) by means of triphenylphosphine in refluxing CCl4 gives the chloro derivative (IV), which is finally desilylated with 40% HF in acetonitrile at room temperature.

参考文献No.457485
标题:SDZ-ASM-981
作者:Graul, A.; Casta馿r, J.
来源:Drugs Fut 1998,23(5),508
合成路线图解说明:

The silylation of the known compound FK-520 by means of tert-butyldimethylsilyl chloride (TBDMS-Cl) and imidazole in DMF gives the disilylated compound (II), which is selectively monodesilylated by means of 40% HF in acetonitrile for 2 h at 0 C yielding the monosilylated compound (III). The chlorination of (III) by means of triphenylphosphine in refluxing CCl4 gives the chloro derivative (IV), which is finally desilylated with 40% HF in acetonitrile at room temperature.

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