摘要
(S)-苹果酸经羟基保护并脱水得(S)-2-乙酰氧基丁二酸酐,经傅-克酰化反应、钯炭催化还原后成乙酯得(S)-2-羟基-4-苯丁酸乙酯,与三氟甲磺酸酐成酯后,与L-丙氨酸苄酯发生取代反应,最后氢化脱苄制得(R,S)-N-(1-乙氧羰基)-3-苯丙基-L-丙氨酸,总收率约30%。
(R,S)-N-(1-Ethoxycarbonyl)-3-phenylpropyl-L-alanine was synthesized from (S)-malic acid by hydroxyl protection and dehydration to give (S)-2-acetoxysuccinic anhydride, which was subjected to Friedel-Crafts acylation reaction, reduction, esterification, substitution and then debenzylation with an overall yield of about 30 %.
出处
《中国医药工业杂志》
CAS
CSCD
北大核心
2013年第8期749-751,共3页
Chinese Journal of Pharmaceuticals