| 摘要 |
<p>The invention herein is directed to a process for the preparation of ethyl 3S-amino-4-pentynoate which involves treating 3-(trimethylsilyl)-2-propynal with L-phenylglycinol in toluen to produce αS-[[3-(trimethylsilyl)-2-propynyliden]amino]benzenethanol; reacting αS-[[3-(trimethylsilyl)-2-propynylidene]amino]benzenethanol with BrZnCH2CO2t-Bu in THF/NMP to produce 1,1-dimethylethyl 3S[(2-hydroxy-1S-phenylethyl)amino]-5-(trimethylsilyl)-4-pentynoate; reacting the 1,1-dimethylethyl 3S-[(2-hydroxy-1S-phenylethyl)amino]-5-(trimethylsilyl)-4-pentynoate with sodium periodate to form 1,1-dimethylethyl 3S-[(phenylmethylene)amino]-5-(trimethylsilyl)-4-pentynoate; hydrolizing 1,1-dimethylethyl 3S-[(phenylmethylene)amino]-5-(trimethylsilyl)-4-pentynoate to produce 1,1-dimethylethyl 3S-amino-5-(trimethylsilyl)-4-pentynoate; transesterifying 1,1-dimethyl 3S-amino-5-(trimethylsilyl)-4-pentynoate and desilylating to produce ethyl 3S-amino-4-pentynoate. The present invention relates also to a process for the preparation of chiral beta-amino acids of formula (I).</p> |
