CAS: 201856-53-3; (3R,4S)-1-Benzoyl-3-(1-Ethoxyethoxy)-4-Phenylazetidin-2-One

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CAS号98-88-4 苯甲酰氯 | CAS号201856-48-6 (3R,4S)-3-(1-乙氧... | CAS号75-75-2 甲基磺酸 | CAS号132127-34-5 (3R4S)-3-羟基-4-苯... | CAS号109-92-2 乙烯基乙醚 | CAS号17599-61-0 N-三甲基硅基苯甲醛亚胺 | CAS号100-52-7 苯甲醛 | CAS号132127-31-2 (3R,4S)-3-triis...

(3R,4S)-3-羟基-4-苯基-2-氮杂环丁酮置于4-二甲氨基吡啶,三乙胺体系中,用 四氢呋喃,二氯甲烷 用作溶剂,化学反应 4.0H,反应生成(3R,4S)-1-苯甲酰-3-(1-乙氧乙氧基)-4-苯基-2-氮杂环丁酮
参考文献:β-内酰胺合成子法高效合成紫杉醇及其c-13侧链类似物的新方法
标题:β-内酰胺合成子法高效合成紫杉醇及其c-13侧链类似物的新方法
摘要:高效手性酯烯酸酯-亚胺缩合可产生具有优异对映体纯度的3-羟基-4-芳基-β-内酰胺,已成功用于对映体纯紫杉醇c-13侧链n-苯甲酰基-(2 R,3 S)-3-苯基-异丝氨酸及其类似物.易于衍生自3-羟基-4-苯基-β-内酰胺的(3 R,4 S)-N-苯甲酰基-3-(1-乙氧基乙氧基)-4-苯基-2-氮杂环丁酮与受保护的浆果赤霉素iii偶联,然后通过脱保护得到光学纯的紫杉醇和高产率的10-脱乙酰基7,10-双(troc)-紫杉醇.完全分配的1 H,13显示并讨论了由此合成的紫杉醇的c和2D(cosy和hetcor)NMR光谱.
Doi:10.1016/s0040-4020(01)91210-4

专利信息

专利号:US-5300638-A
优先权日:1991-07-31
标题:Asymmetric synthesis of taxol side chain
发明人：FARINA VITTORIO; HAUCK SHEILA I
权利人:BRISTOL MYERS SQUIBB CO
摘要:The present invention relates to a process for the preparation of (3R, 4S)-3-hydroxy-4-phenyl-2-azetidinone derivatives which are useful intermediates in the synthesis of taxol from baccatin III, said process comprises reacting an acyloxyacetyl halide with an imine derived from L-threonine; and to compounds of formula (III) which are produced in said process: ##STR1## wherein Ar is phenyl; R 1 is hydrogen, an acyl radical of a carboxylic acid, or a carbonic acid ester radical; R 2 is hydrogen or a carboxy protecting group; and R 3 is hydrogen or a hydroxy protecting group.

专利号:US-5015744-A
优先权日:1989-11-14
标题:Method for preparation of taxol using an oxazinone
发明人：HOLTON ROBERT A
权利人:UNIV FLORIDA STATE
摘要:Process for the preparation of a taxol intermediate comprising contacting an alcohol with an oxazinone having the formula: wherein R1 is aryl, substituted aryl, alkyl, alkenyl, or alkynyl; R2 is hydrogen, ethoxyethyl, 2,2,2-trichloroethoxymethyl or other hydroxyl protecting group; and R3 is aryl, substituted aryl, alkyl, alkenyl, or alkynyl; the contacting of said alcohol and oxazinone being carried out in the presence of a sufficient amount of an activating agent under effective conditions to cause the oxazinone to react with the alcohol to form a beta -amido ester which is suitable for use as an intermediate in the synthesis of taxol.

专利号:CN-1069028-A
优先权日:1991-07-31
标题 :Asymmetric Synthesis of Taxol Side Chain

专利号:EP-0525589-A1
优先权日:1991-07-31
标题:Asymmetric synthesis of taxol side chain