(d)-2-tert-Butoxycarbonylamino-5,5-difluoro-5-phenyl-pentanoic...

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(d)-2-tert-Butoxycarbonylamino-5,5-difluoro-5-phenyl-pentanoic acid: Synthesis and incorporation into the growth hormone secretagogues.
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The first enantioselective synthesis of (d)-2-tert-butoxycarbonylamino-5,5-difluoro-5-phenyl-pentanoic acid 3 was achieved. The incorporation of the titled compound into growth hormone secretagogue (GHS) compounds resulted in new analogs 10 and 16, both of which had significantly increased in vitro potency. The compound 10 also showed improved in vivo efficacy as well as pharmacokinetic properties in rat models.
Li J, Chen SY, Murphy BJ, Flynn N, Seethala R, Slusarchyk D, Yan M, Sleph P, Zhang H, Humphreys WG, Ewing WR, Robl JA, Gordon D, and Tino JA
Bioorganic & medicinal chemistry letters 18(14):4072-4, 2008 Jul 15 - Who cited this? | PubMed ID: 18554903 | Fulltext
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