tert-Butyl （R）-3-amino-3-（3-fluorophenyl）propanoate（5） was prepared with conventional debenzylation method. However, the tert-butyl （R）-3-[（S）-1-phenylethyl-amino]-3-（3-fluorophenyl） propanoate（6） and te...tert-Butyl （R）-3-amino-3-（3-fluorophenyl）propanoate（5） was prepared with conventional debenzylation method. However, the tert-butyl （R）-3-[（S）-1-phenylethyl-amino]-3-（3-fluorophenyl） propanoate（6） and tert-butyl （R）-3-amino-3-phenylpropanoate（7） were generated as the byproducts under the general catalytic hydrogenation Pd（OH）2/C-H2 conditions. So a series of experiments was performed to optimize the reaction conditions so that product 5 could be obtained with high purity and yield. Finally an effective catalytic system, Pd/C-HCOOH-CH3OH, was discovered.展开更多
基金Supported by the National Key New Drug Creation Program of China(No.2009ZX09103-001)the Jiangsu Key Laboratory of Molecular Targeted Antitumor Drug Research Foundation China(No.BM2008201)
文摘tert-Butyl （R）-3-amino-3-（3-fluorophenyl）propanoate（5） was prepared with conventional debenzylation method. However, the tert-butyl （R）-3-[（S）-1-phenylethyl-amino]-3-（3-fluorophenyl） propanoate（6） and tert-butyl （R）-3-amino-3-phenylpropanoate（7） were generated as the byproducts under the general catalytic hydrogenation Pd（OH）2/C-H2 conditions. So a series of experiments was performed to optimize the reaction conditions so that product 5 could be obtained with high purity and yield. Finally an effective catalytic system, Pd/C-HCOOH-CH3OH, was discovered.
