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A total synthesis of (±)-triophamine

 

作者: Edward Piers,   J. Michael Chong,   Kirk Gustafson,   Raymond J. Andersen,  

 

期刊: Canadian Journal of Chemistry  (NRC Available online 1984)
卷期: Volume 62, issue 1  

页码: 1-5

 

ISSN:0008-4042

 

年代: 1984

 

DOI:10.1139/v84-001

 

出版商: NRC Research Press

 

数据来源: NRC

 

摘要:

Treatment of ethyl 2-pentynoate (14) with lithium (phenylthio)(tri-n-butylstannyl)cuprate (12) afforded, in 76% yield, ethyl (Z)-3-(tri-n-butylstannyl)-2-pentenoate (15). On the other hand, when compound14was allowed to react with the (tri-n-butylstannyl)copper reagent13, ethyl (E)-3-(tri-n-butylstannyl)-2-pentenoate (21) was produced in 83% yield. Reduction (diisobutylaluminum hydride, ether) of the esters15and21gave the alcohols16and22, respectively. Treatment of each of the latter substances with pyridine – sulfur trioxide complex, followed by further reduction of the resultant intermediates with lithium aluminum hydride, provided the geometrically isomeric alkenylstannanes17and23. Conjugate addition of (E)-3-lithio-2-pentene (18) (formed by transmetalation of17) to compound19produced the olefinic trimethylhydrazide20, which was converted (diisobutylaluminum hydride, ether; pyridinium dichromate, dimethylformamide) into the corresponding carboxylic acid2. Subjection of compound23to a sequence of reactions identical with that used for the conversion of17into2provided the isomeric acid3, which was identical (infrared,1H nmr) with the natural acid derived from triophamine (1). Conversion of3into thep-nitrophenyl ester26, followed by condensation of the latter substance with guanidine, afforded a chromatographically separable mixture of (±)-triophamine (1) and the corresponding diastereomer.

 

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