广州化工
廣州化工
엄주화공
GUANGZHOU CHEMICAL INDUSTRY AND TECHNOLOGY
2012年
10期
64-65
,共2页
Fmoc-N-甲基-L-苯丙氨酸%微波辐射%合成
Fmoc-N-甲基-L-苯丙氨痠%微波輻射%閤成
Fmoc-N-갑기-L-분병안산%미파복사%합성
N-Fmoc-N-Me-L-Phe%microwave radiation%synthesis
以Fmoc保护的L-苯丙氨酸为起始原料,经恶唑烷酮中间体,在三氟乙酸和无水AlCl3共同催化下,三乙基硅烷还原得到Fmoc保护的N-甲基L-苯丙氨酸,总收率82%。反应过程中,采用微波辐射代替传统的加热方式,缩短了时间,提供了产率,三氟乙酸和无水三氯化铝共同催化体系避免了副产物Fmoc-Tic-OH的生成,该方法优化了生产工艺,缩短了反应时间,节约了原料。
以Fmoc保護的L-苯丙氨痠為起始原料,經噁唑烷酮中間體,在三氟乙痠和無水AlCl3共同催化下,三乙基硅烷還原得到Fmoc保護的N-甲基L-苯丙氨痠,總收率82%。反應過程中,採用微波輻射代替傳統的加熱方式,縮短瞭時間,提供瞭產率,三氟乙痠和無水三氯化鋁共同催化體繫避免瞭副產物Fmoc-Tic-OH的生成,該方法優化瞭生產工藝,縮短瞭反應時間,節約瞭原料。
이Fmoc보호적L-분병안산위기시원료,경악서완동중간체,재삼불을산화무수AlCl3공동최화하,삼을기규완환원득도Fmoc보호적N-갑기L-분병안산,총수솔82%。반응과정중,채용미파복사대체전통적가열방식,축단료시간,제공료산솔,삼불을산화무수삼록화려공동최화체계피면료부산물Fmoc-Tic-OH적생성,해방법우화료생산공예,축단료반응시간,절약료원료。
Fmoc-protected N-methyl-L-phenylalanine was synthesized under the presence of trifluoroacetic acid and anhydrous aluminum chloride as catalyzer and the triethylsilane as reduction,in which the Fmoc-protected L-phenylalanine was used as original material,passing though the genarated intermediate 5-oxazolidinone with microwave assisted heating method.The result showed that using the microwave assisted heating method,the reaction time greatly reduced and the mean total yield increased to 82%,and the composite catalyzer of trifluoroacetic acid and anhydrous aluminum chloride could avoid generating the by-product Fmoc-Tic-OH and save original material.
