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Org Lett ; 3(5): 671-4, 2001 Mar 08.
Article in English | MEDLINE | ID: mdl-11259033

ABSTRACT

[structure: see text]. The NK-1 receptor antagonist 1 has been prepared in seven steps from phenylglycine methyl ester. The key steps are a double ring closing metathesis reaction of tetraene 7 to prepare spirocycle 6 and a reductive Heck reaction to introduce the aryl moiety. This latter reaction discriminates the olefins of compound 6 and proceeds in a highly regio- and stereoselective manner.


Subject(s)
Aza Compounds/chemical synthesis , Neurokinin-1 Receptor Antagonists , Spiro Compounds/chemical synthesis , Aza Compounds/pharmacology , Hydrogenation , Spiro Compounds/pharmacology , Stereoisomerism
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