Asymmetric Synthesis of an Endothelin Receptor Antagonist.
نویسندگان
چکیده
منابع مشابه
Asymmetric synthesis of a selective endothelin A receptor antagonist.
An asymmetric synthesis of a selective endothelin A receptor antagonist 1b is described. Asymmetric conjugate addition of aryllithium derived from 18 to the chiral oxazoline 17 followed by hydrolysis afforded 15 in 96% ee via purification as (S)-(-)-1-phenylethylamine salt. Pd(OAc)(2)/dppf (1,1'-bis(diphenylphosphino)ferrocene) catalyzed carbonylation followed by chemoselective addition of aryl...
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BACKGROUND The role of endothelin (ET)-1 in maintenance of basal vascular tone has been demonstrated by local and systemic vasodilatation to endothelin receptor antagonists in humans. Although the constrictor effects mediated by the vascular smooth muscle ET(A) receptors are clear, the contribution from endothelial and vascular smooth muscle ET(B) receptors remains to be defined. The present st...
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The asymmetric synthesis of L-699,392, a leukotriene antagonist, is reported. The main framework of the molecule is formed via a Heck reaction. The introduction of the asymmetric center was accomplished by the chiral reduction of prochiral ketone using B-chlorodiisopinocampheylborane. A very high asymmetric amplification was observed in which 95% ee product can be obtained from 70% optically pu...
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ژورنال
عنوان ژورنال: Journal of Synthetic Organic Chemistry, Japan
سال: 1999
ISSN: 0037-9980,1883-6526
DOI: 10.5059/yukigoseikyokaishi.57.1016