-药物合成数据库

【药物名称】

化学结构式(Chemical Structure):

参考文献No.	43944
标题:	Substd. heterocyclic acyl-tripeptides useful as thrombin receptor modulators
作者:	Hawkins, M.J.; Maryanoff, B.E.; McComsey, D.F. (Ortho-McNeil Pharmaceutical, Inc.)
来源:	WO 0035942

合成路线图解说明: The compound was prepared via solid-phase synthesis using Rink-amide resin (I). After initial Fmoc-deprotection of (I) with piperidine in DMF, Fmoc-L-phenylalanine (II) was coupled to the resin by means of N,N'-diisopropyl carbodiimide (DIC) and hydroxybenzotriazole (HOBt) in DMF, yielding the phenylalanine-linked resin (III). Subsequent Fmoc-deprotection and coupling cycles with protected arginine (IV) and cyclohexylalanine (VI) produced the peptide resins (V) and (VII), respectively. Further deprotection of (VII) with piperidine, followed by coupling with 5-bromonicotinic acid (VIII) gave the corresponding amide (IX). Cleavage of the final peptide amide from the resin (IX) was then accomplished by treatment trifluoroacetic acid and anisole.

参考文献No.	538401
标题:	Heterocycle-peptide hybrid compounds. Aminotriazole-containing agonists of the thrombin receptor (PAR-1)
作者:	McComsey, D.F.; Hawkins, M.J.; Andrade-Gordon, P.; Addo, M.F.; Oksenberg, D.; Maryanoff, B.E.
来源:	Bioorg Med Chem Lett 1999,9(10),1423

合成路线图解说明: The compound was prepared via solid-phase synthesis using Rink-amide resin (I). After initial Fmoc-deprotection of (I) with piperidine in DMF, Fmoc-L-phenylalanine (II) was coupled to the resin by means of N,N'-diisopropyl carbodiimide (DIC) and hydroxybenzotriazole (HOBt) in DMF, yielding the phenylalanine-linked resin (III). Subsequent Fmoc-deprotection and coupling cycles with protected arginine (IV) and cyclohexylalanine (VI) produced the peptide resins (V) and (VII), respectively. Further deprotection of (VII) with piperidine, followed by coupling with 5-bromonicotinic acid (VIII) gave the corresponding amide (IX). Cleavage of the final peptide amide from the resin (IX) was then accomplished by treatment trifluoroacetic acid and anisole.