路线1:以(1R,4S)-4-((叔丁氧羰基)氨基)环戊-2-烯甲酸为起始原料制备(1S,3R)-3-((叔丁氧基羰基)氨基)环戊烷甲酸
- 步骤:将(1R,4S)-4-((叔丁氧羰基)氨基)环戊-2-烯甲酸(230g,1.0mol)与10%Pd/C催化剂(5.0g)置于500mL甲醇中,在Parr振荡器上于50psi氢气压力下氢化1小时;反应完成后,过滤移除催化剂,蒸发滤液去除溶剂;将残余物溶解于二氯甲烷中,加入无水硫酸钠干燥;再次过滤后,蒸发滤液并真空干燥,得到产物。
- 收率:230g,收率99%
- 表征:经LC-MS分析,C11H19NO4的[M+H+]计算值为230,实测值为230,与预期相符。
- 参考文献:[1] Patent: WO2004/76411, 2004, A2. Location in patent: Page 28;[2] Patent: WO2003/93231, 2003, A2. Location in patent: Page/Page column 56;[3] Patent: US2007/155731, 2007, A1. Location in patent: Page/Page column 27; 36;[4] Patent: WO2005/110409, 2005, A2. Location in patent: Page/Page column 30;[5] Patent: WO2005/75426, 2005, A1. Location in patent: Page/Page column 28