Author/Authors :
Barfoot، نويسنده , , Christopher and Brooks، نويسنده , , Gerald and Davies، نويسنده , , David T. and Elder، نويسنده , , John and Giordano، نويسنده , , Ilaria and Hennessy، نويسنده , , Alan and Jones، نويسنده , , Graham and Markwell، نويسنده , , Roger and McGuire، نويسنده , , Michael F. Miles، نويسنده , , Timothy and Pearson، نويسنده , , Neil and Spoors، نويسنده , , Grant and Sudini، نويسنده , , Ravinder and، نويسنده ,
Abstract :
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 issues were also encountered upon scaling some of the routes. The merits of the diverse routes are assessed and the reasoning given for which one was ultimately used for large-scale synthesis of 1.