Mono N-arylation of piperazine(III): metal-catalyzed N-arylation and its application to the novel preparations of the antifungal posaconazole and its advanced intermediate
โ Scribed by Michael Hepperle; Jeffrey Eckert; Dinesh Gala; Lan Shen; C Anderson Evans; Andrew Goodman
- Book ID
- 104250975
- Publisher
- Elsevier Science
- Year
- 2002
- Tongue
- French
- Weight
- 121 KB
- Volume
- 43
- Category
- Article
- ISSN
- 0040-4039
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โฆ Synopsis
A novel application of Pd 0 -catalyzed arylation to mono N-arylated piperazines, its mechanism, and its application towards the novel syntheses of the key differentially N,N%-diarylated piperazine antifungal intermediate N-(4-hydroxyphenyl)-N%-(4-aminophenyl)piperazine 5 as well as posaconazole 1 are described.
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## Abstract magnified image Inexpensive copper catalysts allow for efficient syntheses of __N__โarylโ, __N__โacylโ, or __N__โHโ(aza)indoles starting from __ortho__โalkynylbromoarenes. The broad scope of this domino __N__โarylation/hydroamin(d)ation process is highlighted by the synthesis of highly
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