The design of efficient and selective routes to pyridyl analogues of 2,3-dihydro-1,4-benzodioxin-6-carbaldehyde
โ Scribed by Christopher W. Barfoot; Pamela Brown; Steven Dabbs; David T. Davies; Alan J. Hennessy; Timothy J. Miles; Neil D. Pearson
- Book ID
- 104098118
- Publisher
- Elsevier Science
- Year
- 2010
- Tongue
- French
- Weight
- 523 KB
- Volume
- 51
- Category
- Article
- ISSN
- 0040-4039
No coin nor oath required. For personal study only.
โฆ Synopsis
This Letter describes the synthetic routes to challenging pyridyl analogues of 2,3-dihydro-1,4-benzodioxin-6-carbaldehyde which were key intermediates for our antibacterial medicinal chemistry programme. All routes described started from kojic acid (8) and have been used to give multigram quantities of each aldehyde.
๐ SIMILAR VOLUMES
This Letter describes the synthesis of challenging pyridyl analogues of 3-oxo-3,4-dihydro-2H-1,4-(benzothiazine or benzoxazine)-6-carbaldehydes. The six different routes described are high yielding, contain no major purification issues and have been used to give gram quantities of each aldehyde.
This Letter describes the synthetic challenges in synthesising key 1,4-cis-substituted cyclohexylamide intermediate 1 for our research programme. Five different routes address the major issues of selectivity to afford the cis product in isomerically pure form and in high yield. Major purification is