The solid phase synthesis of complex propargylamines using the combination of Sonogashira and Mannich reactions

Tetrahedron Letters

Volumn 39, Issue 22, 1998, Pages 3647-3650

  Dyatkin, Alexey B ^a   Rivero, Ralph A ^a  

^a JOHNSON AND JOHNSON PHARMACEUTICAL RESEARCH AND DEVELOPMENT   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

IODOBENZOIC ACID DERIVATIVE; N (1 INDENYL) N METHYL N PROPARGYLAMINE;

ARTICLE; CATALYST; COMPLEX FORMATION; DRUG SYNTHESIS; NONHUMAN; REACTION ANALYSIS; SIALYLATION; SOLID PHASE EXTRACTION;

EID: 0032575168     PISSN: 00404039     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0040-4039(98)00639-X     Document Type: Article

References (17)

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15. 7. We investigated the reaction of different aldehydes with polymer-supported acetylene carboxylates and amines. Substituted benzaldehydes, aryl acetaldehydes, heteroaryl aldehydes as well as cyclic and non-cyclic secondary amines were successfully used in this transformation. The scope and limitations of the condensation will be presented in a future publication.
16. 8. The purity of the condensation products with piperidines and non-cyclic secondary amines was usually more than 85%. In the tetrahydroisoquinoline case (7), the purity of the crude (direct from cleavage) product was 40 - 60% by HPLC.
17. +).